-
1
-
-
14944352553
-
New anti-HIV agents in preclinical or clinical development
-
De Clercq, E. New anti-HIV agents in preclinical or clinical development. Front. Med. Chem. 2004, 1, 543-579.
-
(2004)
Front. Med. Chem.
, vol.1
, pp. 543-579
-
-
De Clercq, E.1
-
2
-
-
0036436747
-
CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor
-
Vermeire, K.; Zhang, Y.; Princen, K.; Hatse, S.; Samala, M. F.; Dey, K.; Choi, H.-J.; Ahn, Y.; Sodoma, A.; Snoeck, R.; Andrei, G.; De Clercq, E.; Bell, T. W.; Schols, D. CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor. Virology 2002, 302, 342-353.
-
(2002)
Virology
, vol.302
, pp. 342-353
-
-
Vermeire, K.1
Zhang, Y.2
Princen, K.3
Hatse, S.4
Samala, M.F.5
Dey, K.6
Choi, H.-J.7
Ahn, Y.8
Sodoma, A.9
Snoeck, R.10
Andrei, G.11
De Clercq, E.12
Bell, T.W.13
Schols, D.14
-
3
-
-
0037220770
-
The anti-HIV potency of cyclotriazadisulfonamide analogs is directly correlated with their ability to down-modulate the CD4 receptor
-
Vermeire, K; Bell, T. W.; Choi, H.-J.; Jin, Q.; Samala, M. F.; Sodoma, A.; De Clercq, E.; Schols, D. The anti-HIV potency of cyclotriazadisulfonamide analogs is directly correlated with their ability to down-modulate the CD4 receptor. Mol. Pharmacol. 2003, 63, 203-210.
-
(2003)
Mol. Pharmacol.
, vol.63
, pp. 203-210
-
-
Vermeire, K.1
Bell, T.W.2
Choi, H.-J.3
Jin, Q.4
Samala, M.F.5
Sodoma, A.6
De Clercq, E.7
Schols, D.8
-
4
-
-
7744237428
-
CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro
-
Vermeire, K.; Princen, K.; Hatse, S.; De Clercq, E.; Dey, K.; Bell, T. W.; Schols, D. CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro. AIDS 2004, 18, 2115-2125.
-
(2004)
AIDS
, vol.18
, pp. 2115-2125
-
-
Vermeire, K.1
Princen, K.2
Hatse, S.3
De Clercq, E.4
Dey, K.5
Bell, T.W.6
Schols, D.7
-
5
-
-
4644227155
-
Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection
-
Balzarini, J.; Hatse, S.; Vermeire, K.; Princen, K.; Aquaro, S.; Perno, C.-F.; De Clercq, E.; Egberink, H.; Vanden Mooter, G.; Peumans, W.; Van Damme, E.; Schols, D. Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection. Antimicrob. Agents Chemother. 2004, 48, 3858-3870.
-
(2004)
Antimicrob. Agents Chemother.
, vol.48
, pp. 3858-3870
-
-
Balzarini, J.1
Hatse, S.2
Vermeire, K.3
Princen, K.4
Aquaro, S.5
Perno, C.-F.6
De Clercq, E.7
Egberink, H.8
Vanden Mooter, G.9
Peumans, W.10
Van Damme, E.11
Schols, D.12
-
6
-
-
4544256598
-
Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins
-
Balzarini, J.; Van Laethem, K.; Hatse, S.; Vermeire, K.; De Clercq, E.; Peumans, W.; Van Damme, E.; Vandamme, A.-M.; Böhlmstedt, A.; Schols, D. Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins. J. Virol. 2004, 78, 10617-10627.
-
(2004)
J. Virol.
, vol.78
, pp. 10617-10627
-
-
Balzarini, J.1
Van Laethem, K.2
Hatse, S.3
Vermeire, K.4
De Clercq, E.5
Peumans, W.6
Van Damme, E.7
Vandamme, A.-M.8
Böhlmstedt, A.9
Schols, D.10
-
7
-
-
0030790094
-
Discovery of cyanovirin-N, a novel human immunodeficiency virus-inactivating protein that binds viral surface envelope glycoprotein gp120: Potential applications to microbicide development
-
Boyd, M. R.; Gustafson, K. R.; McMahon, J. B.; Shoemaker, R. H.; O'Keefe, B. R.; Mori, T.; Gulakowski, R. J.; Wu, L.; Rivera, M. I.; Laurencot, C. M.; Currens, M. J.; Cardellina, J. H., II; Buckheit, R. W., Jr.; Nara, P. L.; Pannell, L. K.; Sowder, R. C., II; Henderson, L. E. Discovery of cyanovirin-N, a novel human immunodeficiency virus-inactivating protein that binds viral surface envelope glycoprotein gp120: potential applications to microbicide development. Antimicrob. Agents Chemother. 1997, 41, 1521-1530.
-
(1997)
Antimicrob. Agents Chemother.
, vol.41
, pp. 1521-1530
-
-
Boyd, M.R.1
Gustafson, K.R.2
McMahon, J.B.3
Shoemaker, R.H.4
O'Keefe, B.R.5
Mori, T.6
Gulakowski, R.J.7
Wu, L.8
Rivera, M.I.9
Laurencot, C.M.10
Currens, M.J.11
Cardellina II, J.H.12
Buckheit Jr., R.W.13
Nara, P.L.14
Pannell, L.K.15
Sowder II, R.C.16
Henderson, L.E.17
-
8
-
-
0035112229
-
Cyanovirin-N, a potent human immunodeficiency virus-inactivating protein, blocks both CD4-dependent and CD4-independent binding of soluble gp120 (sgp120) to target cells, inhibits sCD4-induced binding of sgp120 to cell-associated CXCR4, and dissociates bound sgp120 from target cells
-
Mori, T.; Boyd, M. R. Cyanovirin-N, a potent human immunodeficiency virus-inactivating protein, blocks both CD4-dependent and CD4-independent binding of soluble gp120 (sgp120) to target cells, inhibits sCD4-induced binding of sgp120 to cell-associated CXCR4, and dissociates bound sgp120 from target cells. Antimicrob. Agents Chemother. 2001, 45, 664-672.
-
(2001)
Antimicrob. Agents Chemother.
, vol.45
, pp. 664-672
-
-
Mori, T.1
Boyd, M.R.2
-
9
-
-
0037300816
-
Cyanovirin-N: A sugar-binding antiviral protein with a new twist
-
Botos, I.; Wlodawer, A. Cyanovirin-N: a sugar-binding antiviral protein with a new twist. Cell. Mol. Life Sci. 2003, 60, 277-287.
-
(2003)
Cell. Mol. Life Sci.
, vol.60
, pp. 277-287
-
-
Botos, I.1
Wlodawer, A.2
-
10
-
-
0038454664
-
Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics
-
Balzarini, J.; Pannecouque, C.; De Clercq, E.; Pavlov, A. Y.; Printsevskaya, S. S.; Miroshnikova, O. V.; Reznikova, M. I.; Preobrazhenskaya, M. N. Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics. J. Med. Chem. 2003, 46, 2755-2764.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 2755-2764
-
-
Balzarini, J.1
Pannecouque, C.2
De Clercq, E.3
Pavlov, A.Y.4
Printsevskaya, S.S.5
Miroshnikova, O.V.6
Reznikova, M.I.7
Preobrazhenskaya, M.N.8
-
11
-
-
0141680855
-
Discovery of 4-benzoyl-1-[(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl) oxoacetyl]-2-(R)-methylpiperazine (BMS-378806): A novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions
-
Wang, T.; Zhang, Z.; Wallace, O. B.; Deshpande, M.; Fang, H.; Yang, Z.; Zadjura, L. M.; Tweedie, D. L.; Huang, S.; Zhao, F.; Ranadive, S.; Robinson, B. S.; Gong, Y.-F.; Ricarrdi, K.; Spicer, T. P.; Deminie, C.; Rose, R.; Wang, H.-G. H.; Blair, W. S.; Shi, P.-Y.; Lin, P.-f.; Colonno, R. J.; Meanwell, N. A. Discovery of 4-benzoyl-1-[(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J. Med. Chem. 2003, 46, 4236-4239.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4236-4239
-
-
Wang, T.1
Zhang, Z.2
Wallace, O.B.3
Deshpande, M.4
Fang, H.5
Yang, Z.6
Zadjura, L.M.7
Tweedie, D.L.8
Huang, S.9
Zhao, F.10
Ranadive, S.11
Robinson, B.S.12
Gong, Y.-F.13
Ricarrdi, K.14
Spicer, T.P.15
Deminie, C.16
Rose, R.17
Wang, H.-G.H.18
Blair, W.S.19
Shi, P.-Y.20
Lin, P.-F.21
Colonno, R.J.22
Meanwell, N.A.23
more..
-
12
-
-
0141856289
-
Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions
-
Guo, Q.; Ho, H.-T.; Dicker, I.; Fan, L.; Zhou, N.; Friborg, J.; Wang, T.; McAuliffe, B. V.; Wang, H.-g. H.; Rose, R. E.; Fang, H.; Scarnati, H. T.; Langley, D. R.; Meanwell, N. A.; Abraham, R.; Colonno, R. J.; Lin, P.-f. Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J. Virol. 2003, 77, 10528-10536.
-
(2003)
J. Virol.
, vol.77
, pp. 10528-10536
-
-
Guo, Q.1
Ho, H.-T.2
Dicker, I.3
Fan, L.4
Zhou, N.5
Friborg, J.6
Wang, T.7
McAuliffe, B.V.8
Wang, H.-G.H.9
Rose, R.E.10
Fang, H.11
Scarnati, H.T.12
Langley, D.R.13
Meanwell, N.A.14
Abraham, R.15
Colonno, R.J.16
Lin, P.-F.17
-
13
-
-
0141703204
-
A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding
-
Lin, P.-F.; Blair, W.; Wang, T.; Spicer, T.; Guo, Q.; Zhou, N.; Gong, Y.-F.; Wang, H.-G. H.; Rose, R.; Yamanaka, G.; Robinson, B.; Li, C.-B.; Fridell, R.; Deminie, C.; Demers, G.; Yang, Z.; Zadjura, L.; Meanwell, N.; Colonno, R. A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding. Proc. Natl. Acad. Sci. U.S.A. 2003, 100, 11013-11018
-
(2003)
Proc. Natl. Acad. Sci. U.S.A.
, vol.100
, pp. 11013-11018
-
-
Lin, P.-F.1
Blair, W.2
Wang, T.3
Spicer, T.4
Guo, Q.5
Zhou, N.6
Gong, Y.-F.7
Wang, H.-G.H.8
Rose, R.9
Yamanaka, G.10
Robinson, B.11
Li, C.-B.12
Fridell, R.13
Deminie, C.14
Demers, G.15
Yang, Z.16
Zadjura, L.17
Meanwell, N.18
Colonno, R.19
-
14
-
-
14944368876
-
BMS-488043: A novel, small-molecule HIV-1 attachment inhibitor
-
Toulon, France, June 3-5; Abstract OP 4.6
-
Colonno, R.; Ho, H.; Zhou, N.; Masterson, T.; Hanna, G.; Kadow, J.; Lin, P.-F. BMS-488043: a novel, small-molecule HIV-1 attachment inhibitor. Presented at the 13th International Symposium on HIV & Emerging Infectious Diseases, Toulon, France, June 3-5, 2004; Abstract OP 4.6, p 58.
-
(2004)
13th International Symposium on HIV & Emerging Infectious Diseases
, pp. 58
-
-
Colonno, R.1
Ho, H.2
Zhou, N.3
Masterson, T.4
Hanna, G.5
Kadow, J.6
Lin, P.-F.7
-
15
-
-
0038681342
-
The bicyclam AMD3100 story
-
De Clercq, E. The bicyclam AMD3100 story. Nat. Rev. Drug Discovery 2003, 2, 581-587.
-
(2003)
Nat. Rev. Drug Discovery
, vol.2
, pp. 581-587
-
-
De Clercq, E.1
-
16
-
-
0034120373
-
Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR4-chemokine receptor, in human volunteers
-
Hendrix, C. W.; Flexner, C.; MacFarland, R. T.; Giandomenico, C.; Fuchs, E. J.; Redpath, E.; Bridger, G.; Henson, G. W. Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR4-chemokine receptor, in human volunteers. Antimicrob. Agents Chemother. 2000, 44, 1667-1673.
-
(2000)
Antimicrob. Agents Chemother.
, vol.44
, pp. 1667-1673
-
-
Hendrix, C.W.1
Flexner, C.2
MacFarland, R.T.3
Giandomenico, C.4
Fuchs, E.J.5
Redpath, E.6
Bridger, G.7
Henson, G.W.8
-
17
-
-
0011309256
-
AMD-3100, a CXCR4 antagonist, reduced HIV viral load and X4 virus levels in humans
-
AMD-3100 HIV Study Group. Seattle, WA, February 24-28; Abstract 2
-
Schols, D.; Claes, S.; De Clercq, E.; Hendrix, C.; Bridger, G.; Calandra, G.; Henson, G. W.; Fransen, S.; Huang, W; Whitcomb, J. M.; Petropoulos, C. J. AMD-3100 HIV Study Group. AMD-3100, a CXCR4 antagonist, reduced HIV viral load and X4 virus levels in humans. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002; Abstract 2, p 53.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 53
-
-
Schols, D.1
Claes, S.2
De Clercq, E.3
Hendrix, C.4
Bridger, G.5
Calandra, G.6
Henson, G.W.7
Fransen, S.8
Huang, W.9
Whitcomb, J.M.10
Petropoulos, C.J.11
-
18
-
-
0041893844
-
Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist H
-
Boston, MA, February 10-14; Abstract 563
-
Schols, D.; Claes, S.; Hatse, S.; Princen, K.; Vermeire, K.; De Clercq, E.; Skerlj, R.; Bridger, G.; Calandra, G. Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist H. Presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, February 10-14, 2003; Abstract 563.
-
(2003)
10th Conference on Retroviruses and Opportunistic Infections
-
-
Schols, D.1
Claes, S.2
Hatse, S.3
Princen, K.4
Vermeire, K.5
De Clercq, E.6
Skerlj, R.7
Bridger, G.8
Calandra, G.9
-
19
-
-
0041893844
-
Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist
-
Presented at the 16th International Conference on Antiviral Research, Savannah, GA, April 27 to May 1, 2003; Abstract A39, No. 2
-
Schols, D.; Claes, S.; Hatse, S.; Princen, K.; Vermeire, K.; De Clercq, E.; Skerlj, R.; Bridger, G.; Calandra, G. Anti-HIV activity profile of AMD070, an orally bioavailable CXCR4 antagonist. Presented at the 16th International Conference on Antiviral Research, Savannah, GA, April 27 to May 1, 2003; Abstract A39, No. 2; Antiviral Res. 2003, 57, A39.
-
(2003)
Antiviral Res.
, vol.57
-
-
Schols, D.1
Claes, S.2
Hatse, S.3
Princen, K.4
Vermeire, K.5
De Clercq, E.6
Skerlj, R.7
Bridger, G.8
Calandra, G.9
-
20
-
-
4243298153
-
A specific CXCR4 antagonist with potent anti-HIV activity
-
Presented at the 15th International Conference on Antiviral Research, Prague, Czech Republic, March 17-21, 2002; Abstract A36, No. 5
-
Hatse, S.; Princen, K.; Bridger, G.; Skerlj, R.; Henson, G.; De Clercq, E.; Schols, D. A specific CXCR4 antagonist with potent anti-HIV activity. Presented at the 15th International Conference on Antiviral Research, Prague, Czech Republic, March 17-21, 2002; Abstract A36, No. 5; Antiviral Res. 2002, 53, A36.
-
(2002)
Antiviral Res.
, vol.53
-
-
Hatse, S.1
Princen, K.2
Bridger, G.3
Skerlj, R.4
Henson, G.5
De Clercq, E.6
Schols, D.7
-
21
-
-
0037388121
-
A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity
-
Ichiyama, K.; Yokoyama-Kumakura, S.; Tanaka, Y.; Tanaka, R.; Hirose, K.; Bannai, K.; Edamatsu, T.; Yanaka, M.; Niitani, Y.; Miyano-Kurosaki, N.; Takaku, H.; Koyanagi, Y.; Yamamoto, N. A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. U.S.A. 2003, 100, 4185-4190.
-
(2003)
Proc. Natl. Acad. Sci. U.S.A.
, vol.100
, pp. 4185-4190
-
-
Ichiyama, K.1
Yokoyama-Kumakura, S.2
Tanaka, Y.3
Tanaka, R.4
Hirose, K.5
Bannai, K.6
Edamatsu, T.7
Yanaka, M.8
Niitani, Y.9
Miyano-Kurosaki, N.10
Takaku, H.11
Koyanagi, Y.12
Yamamoto, N.13
-
22
-
-
13044256383
-
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
-
Baba, M.; Nishimura, O.; Kanzaki, N.; Okamoto, M.; Sawada, H.; Iizawa, Y.; Shiraishi, M.; Aramaki, Y.; Okonogi, K.; Ogawa, Y.; Meguro, K.; Fujino, M. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. U.S.A. 1999, 96, 5698-5703.
-
(1999)
Proc. Natl. Acad. Sci. U.S.A.
, vol.96
, pp. 5698-5703
-
-
Baba, M.1
Nishimura, O.2
Kanzaki, N.3
Okamoto, M.4
Sawada, H.5
Iizawa, Y.6
Shiraishi, M.7
Aramaki, Y.8
Okonogi, K.9
Ogawa, Y.10
Meguro, K.11
Fujino, M.12
-
23
-
-
0034625144
-
A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5
-
Dragic, T.; Trkola, A.; Thompson, D. A.; Cormier, E. G.; Kajumo, F. A.; Maxwell, E.; Lin, S. W.; Ying, W.; Smith, S. O.; Sakmar, T. P.; Moore, J. P. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. Proc. Natl. Acad. Sci. U.S.A. 2000, 97, 5639-5644.
-
(2000)
Proc. Natl. Acad. Sci. U.S.A.
, vol.97
, pp. 5639-5644
-
-
Dragic, T.1
Trkola, A.2
Thompson, D.A.3
Cormier, E.G.4
Kajumo, F.A.5
Maxwell, E.6
Lin, S.W.7
Ying, W.8
Smith, S.O.9
Sakmar, T.P.10
Moore, J.P.11
-
24
-
-
0041392874
-
Anti-HIV-1 activity of TAK-220, a small molecule CCR5 antagonist
-
Boston, MA, February 10-14; Abstract 11
-
Iizawa, Y.; Kanzaki, N.; Takashima, K.; Miyake, H.; Tagawa, Y.; Sugihara, Y.; Baba, M. Anti-HIV-1 activity of TAK-220, a small molecule CCR5 antagonist. Presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, February 10-14, 2003; Abstract 11.
-
(2003)
10th Conference on Retroviruses and Opportunistic Infections
-
-
Iizawa, Y.1
Kanzaki, N.2
Takashima, K.3
Miyake, H.4
Tagawa, Y.5
Sugihara, Y.6
Baba, M.7
-
25
-
-
14944375586
-
-
(Takeda Chemical Industries Ltd.) Preparation of 1-benzazocine-5- carboxamides and related bicyclic compounds as CCR-5 antagonists for use against HIV infections and other diseases. Patent Application WO-00314105, 2003
-
Shiraishi, M.; Baba, M.; Aikawa, K.; Kanzaki, N.; Seto, M.; Iizawa, Y. (Takeda Chemical Industries Ltd.) Preparation of 1-benzazocine-5-carboxamides and related bicyclic compounds as CCR-5 antagonists for use against HIV infections and other diseases. Patent Application WO-00314105, 2003.
-
-
-
Shiraishi, M.1
Baba, M.2
Aikawa, K.3
Kanzaki, N.4
Seto, M.5
Iizawa, Y.6
-
26
-
-
0035940445
-
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo
-
Strizki, J. M.; Xu, S.; Wagner, N. E.; Wojcik, L.; Liu, J.; Hou, Y.; Endres, M.; Palani, A.; Shapiro, S.; Clader, J. W.; Greenlee, W. J.; Tagat, J. R.; McCombie, S.; Cox, K.; Fawzi, A. B.; Chou, C.-C.; Pugliese-Sivo, C.; Davies, L.; Moreno, M. E.; Ho, D. D.; Trkola, A.; Stoddart, C. A.; Moore, J. P.; Reyes, G. R.; Baroudy, B. M. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc. Natl. Acad. Sci. U.SA. 2001, 98, 12718-12723.
-
(2001)
Proc. Natl. Acad. Sci. U.SA.
, vol.98
, pp. 12718-12723
-
-
Strizki, J.M.1
Xu, S.2
Wagner, N.E.3
Wojcik, L.4
Liu, J.5
Hou, Y.6
Endres, M.7
Palani, A.8
Shapiro, S.9
Clader, J.W.10
Greenlee, W.J.11
Tagat, J.R.12
McCombie, S.13
Cox, K.14
Fawzi, A.B.15
Chou, C.-C.16
Pugliese-Sivo, C.17
Davies, L.18
Moreno, M.E.19
Ho, D.D.20
Trkola, A.21
Stoddart, C.A.22
Moore, J.P.23
Reyes, G.R.24
Baroudy, B.M.25
more..
-
27
-
-
0003339453
-
SCH C: Safety and antiviral effects of a CCR5 receptor antagonist in HIV-1 infected subjects
-
Seattle, WA February 24-28; Abstract 1
-
Reynes, J.; Rouzier, R.; Kanouni, T.; Baillat, V.; Baroudy, B.; Keung, A.; Hogan, C.; Markowitz, M.; Laughlin, M. SCH C: safety and antiviral effects of a CCR5 receptor antagonist in HIV-1 infected subjects. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA February 24-28, 2002; Abstract 1, p 53.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 53
-
-
Reynes, J.1
Rouzier, R.2
Kanouni, T.3
Baillat, V.4
Baroudy, B.5
Keung, A.6
Hogan, C.7
Markowitz, M.8
Laughlin, M.9
-
28
-
-
0037325553
-
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III. Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
-
McCombie, S. W.; Tagat, J. R.; Vice, S. F.; Lin, S.-I.; Steensma, R.; Palani, A.; Neustadt, B. R.; Baroudy, B. M.; Strizki, J. M.; Endres, M.; Cox, K.; Dan, N.; Chou, C.-C. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III. Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. Bioorg. Med. Chem. Lett. 2003, 13, 567-571.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 567-571
-
-
McCombie, S.W.1
Tagat, J.R.2
Vice, S.F.3
Lin, S.-I.4
Steensma, R.5
Palani, A.6
Neustadt, B.R.7
Baroudy, B.M.8
Strizki, J.M.9
Endres, M.10
Cox, K.11
Dan, N.12
Chou, C.-C.13
-
29
-
-
0037294907
-
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: Synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides
-
Palani, A.; Shapiro, S.; Clader, J. W.; Greenlee, W. J.; Vice, S.; McCombie, S.; Cox, K.; Strizki, J.; Baroudy, B. M. Oximino-piperidino- piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides. Bioorg. Med. Chem. Lett. 2003, 13, 709-712.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 709-712
-
-
Palani, A.1
Shapiro, S.2
Clader, J.W.3
Greenlee, W.J.4
Vice, S.5
McCombie, S.6
Cox, K.7
Strizki, J.8
Baroudy, B.M.9
-
30
-
-
0037404511
-
Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry
-
Tsamis, F.; Gravilov, S.; Kajumo, F.; Seibert, C.; Kuhmann, S.; Ketas, T.; Trkola, A.; Palani, A.; Clader, J. W.; Tagat, J. R.; McCombie, S.; Baroudy, B.; Moore, J. P.; Sakmar, T. P.; Dragic, T. Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry. J. Virol. 2003, 77, 5201-5208.
-
(2003)
J. Virol.
, vol.77
, pp. 5201-5208
-
-
Tsamis, F.1
Gravilov, S.2
Kajumo, F.3
Seibert, C.4
Kuhmann, S.5
Ketas, T.6
Trkola, A.7
Palani, A.8
Clader, J.W.9
Tagat, J.R.10
McCombie, S.11
Baroudy, B.12
Moore, J.P.13
Sakmar, T.P.14
Dragic, T.15
-
31
-
-
0035860744
-
Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5
-
Maeda, K.; Yoshimura, K.; Shibayama, S.; Habashita, H.; Tada, H.; Sagawa, K.; Miyakawa, T.; Aoki, M.; Fukushima, D.; Mitsuya, H. Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. J. Biol. Chem. 2001, 276, 35194-35200.
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 35194-35200
-
-
Maeda, K.1
Yoshimura, K.2
Shibayama, S.3
Habashita, H.4
Tada, H.5
Sagawa, K.6
Miyakawa, T.7
Aoki, M.8
Fukushima, D.9
Mitsuya, H.10
-
32
-
-
20144366486
-
Novel HIV-specific spirodiketopiperazine CCR5 inhibitors potent against a wide spectrum of R5-HIV
-
Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 014
-
Maeda, K.; Nakata, H.; Miyakawa, T.; Ogata, H.; Koh, Y.; Takaoka, Y.; Shibayama, S.; Moravek, J.; Koyanagi, Y.; Mitsuya, H. Novel HIV-specific spirodiketopiperazine CCR5 inhibitors potent against a wide spectrum of R5-HIV. Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 014; Antiviral Res. 2002, 15.
-
(2002)
Antiviral Res.
, pp. 15
-
-
Maeda, K.1
Nakata, H.2
Miyakawa, T.3
Ogata, H.4
Koh, Y.5
Takaoka, Y.6
Shibayama, S.7
Moravek, J.8
Koyanagi, Y.9
Mitsuya, H.10
-
33
-
-
0042896003
-
UK-427,857, a novel small molecule HIV entry inhibitor is a specific antagonist of the chemokine receptor CCR5
-
Boston, MA, February 10-14; Abstract 12
-
Dorr, P.; Macartney, M.; Rickett, G.; Smith-Burchnell, C.; Dobbs, S.; Mori, J.; Griffin, P.; Lok, J.; Irvine, R.; Westby, M.; Hitchcock, C.; Stammen, B.; Price, D.; Armour, D.; Wood, A.; Perros, M. UK-427,857, a novel small molecule HIV entry inhibitor is a specific antagonist of the chemokine receptor CCR5. Presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, February 10-14, 2003; Abstract 12, p 62.
-
(2003)
10th Conference on Retroviruses and Opportunistic Infections
, pp. 62
-
-
Dorr, P.1
Macartney, M.2
Rickett, G.3
Smith-Burchnell, C.4
Dobbs, S.5
Mori, J.6
Griffin, P.7
Lok, J.8
Irvine, R.9
Westby, M.10
Hitchcock, C.11
Stammen, B.12
Price, D.13
Armour, D.14
Wood, A.15
Perros, M.16
-
34
-
-
14944368471
-
The discovery and exploratory development of UK-427,857: A novel CCR5 antagonist for the treatment of HIV
-
Toulon, France, June 3-5; Abstract OP 4.5
-
Hitchcock, C. A. The discovery and exploratory development of UK-427,857: a novel CCR5 antagonist for the treatment of HIV. Presented at the 13th International Symposium on HIV & Emerging Infectious Diseases, Toulon, France, June 3-5, 2004; Abstract OP 4.5; p 57.
-
(2004)
13th International Symposium on HIV & Emerging Infectious Diseases
, pp. 57
-
-
Hitchcock, C.A.1
-
35
-
-
0035935205
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: Lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity
-
Hale, J. J.; Budhu, R. J.; Holson, E. B.; Finke, P. E.; Oates, B.; Mills, S. G.; MacCoss, M.; Gould, S. L.; DeMartino, J. A.; Springer, M. S.; Siciliano, S.; Malkowitz, L.; Schleif, W. A.; Hazuda, D.; Miller, M.; Kessler, J.; Danzeisen, R.; Holmes, K.; Lineberger, J.; Carella, A.; Carver, G.; Emini, E. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: Lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity. Bioorg. Med. Chem. Lett. 2001, 11, 2741-2745.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2741-2745
-
-
Hale, J.J.1
Budhu, R.J.2
Holson, E.B.3
Finke, P.E.4
Oates, B.5
Mills, S.G.6
MacCoss, M.7
Gould, S.L.8
Demartino, J.A.9
Springer, M.S.10
Siciliano, S.11
Malkowitz, L.12
Schleif, W.A.13
Hazuda, D.14
Miller, M.15
Kessler, J.16
Danzeisen, R.17
Holmes, K.18
Lineberger, J.19
Carella, A.20
Carver, G.21
Emini, E.22
more..
-
36
-
-
18644374488
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity
-
Hale, J. J.; Budhu, R. J.; Mills, S. G.; MacCoss, M.; Gould, S. L.; DeMartino, J. A.; Springer, M. S.; Siciliano, S. J.; Malkowitz, L.; Schleif, W. A.; Hazuda, D.; Miller, M.; Kessler, J.; Danzeisen, R.; Holmes, K.; Lineberger, J.; Carella, A.; Carver, G.; Emini, E. A. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity. Bioorg. Med. Chem. Lett. 2002, 12, 2997-3000.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2997-3000
-
-
Hale, J.J.1
Budhu, R.J.2
Mills, S.G.3
MacCoss, M.4
Gould, S.L.5
Demartino, J.A.6
Springer, M.S.7
Siciliano, S.J.8
Malkowitz, L.9
Schleif, W.A.10
Hazuda, D.11
Miller, M.12
Kessler, J.13
Danzeisen, R.14
Holmes, K.15
Lineberger, J.16
Carella, A.17
Carver, G.18
Emini, E.A.19
-
37
-
-
18244396143
-
CCR5 antagonists: Bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines
-
Lynch, C. L.; Gentry, A. L.; Hale, J. J.; Mills, S. G.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A.; Siciliano, S. J.; Cascieri, M. A.; Doss, G.; Carella, A.; Carver, G.; Holmes, K.; Schleif, W. A.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Emini, E. A. CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines. Bioorg. Med. Chem. Lett. 2002, 12, 677-679.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 677-679
-
-
Lynch, C.L.1
Gentry, A.L.2
Hale, J.J.3
Mills, S.G.4
MacCoss, M.5
Malkowitz, L.6
Springer, M.S.7
Gould, S.L.8
Demartino, J.A.9
Siciliano, S.J.10
Cascieri, M.A.11
Doss, G.12
Carella, A.13
Carver, G.14
Holmes, K.15
Schleif, W.A.16
Danzeisen, R.17
Hazuda, D.18
Kessler, J.19
Lineberger, J.20
Miller, M.21
Emini, E.A.22
more..
-
38
-
-
18644372005
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV
-
Lynch, C. L.; Hale, J. J.; Budhu, R. J.; Gentry, A. L.; Mills, S. G.; Chapman, K. T.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A.; Siciliano, S. J.; Cascieri, M. A.; Carella, A.; Carver, G.; Holmes, K.; Schleif, W. A.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Emini, E. A. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. Bioorg. Med. Chem. Lett. 2002, 12, 3001-3004.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 3001-3004
-
-
Lynch, C.L.1
Hale, J.J.2
Budhu, R.J.3
Gentry, A.L.4
Mills, S.G.5
Chapman, K.T.6
MacCoss, M.7
Malkowitz, L.8
Springer, M.S.9
Gould, S.L.10
Demartino, J.A.11
Siciliano, S.J.12
Cascieri, M.A.13
Carella, A.14
Carver, G.15
Holmes, K.16
Schleif, W.A.17
Danzeisen, R.18
Hazuda, D.19
Kessler, J.20
Lineberger, J.21
Miller, M.22
Emini, E.A.23
more..
-
39
-
-
0037330767
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains
-
Willoughby, C. A.; Rosauer, K. G.; Hale, J. J.; Budhu, R. J.; Mills, S. G.; Chapman, K. T.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A.; Siciliano, S. J.; Cascieri, M. A.; Carella, A.; Carver, G.; Holmes, K.; Schleif, W. A.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Emini, E. A. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains. Bioorg. Med. Chem. Lett. 2003, 13, 427-431.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 427-431
-
-
Willoughby, C.A.1
Rosauer, K.G.2
Hale, J.J.3
Budhu, R.J.4
Mills, S.G.5
Chapman, K.T.6
MacCoss, M.7
Malkowitz, L.8
Springer, M.S.9
Gould, S.L.10
Demartino, J.A.11
Siciliano, S.J.12
Cascieri, M.A.13
Carella, A.14
Carver, G.15
Holmes, K.16
Schleif, W.A.17
Danzeisen, R.18
Hazuda, D.19
Kessler, J.20
Lineberger, J.21
Miller, M.22
Emini, E.A.23
more..
-
40
-
-
12244267994
-
Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: A molecular modeling-guided mutagenesis study of the binding pocket
-
Castonguay, L. A.; Weng, Y.; Adolfsen, W.; Di Salvo, J.; Kilburn, R.; Caldwell, C. G.; Daugherty, B. L.; Finke, P. E.; Hale, J. J.; Lynch, C. L.; Mills, S. G.; MacCoss, M.; Springer, M. S.; DeMartino, J. A. Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket. Biochemistry 2003, 42, 1544-1550.
-
(2003)
Biochemistry
, vol.42
, pp. 1544-1550
-
-
Castonguay, L.A.1
Weng, Y.2
Adolfsen, W.3
Di Salvo, J.4
Kilburn, R.5
Caldwell, C.G.6
Daugherty, B.L.7
Finke, P.E.8
Hale, J.J.9
Lynch, C.L.10
Mills, S.G.11
MacCoss, M.12
Springer, M.S.13
Demartino, J.A.14
-
41
-
-
10744225125
-
Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection
-
Veazey, R. S.; Klasse, P. J.; Ketas, T. J.; Reeves, J. D.; Piatak, M., Jr.; Kunstman, K.; Kuhmann, S. E.; Marx, P. A.; Lifson, J. D.; Dufour, J.; Mefford, M.; Pandrea, I.; Wolinsky, S. M.; Doms, R. W.; DeMartino, J. A.; Siciliano, S. J.; Lyons, K.; Springer, M. S.; Moore, J. P. Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection. J. Exp. Med. 2003, 198, 1551-1562.
-
(2003)
J. Exp. Med.
, vol.198
, pp. 1551-1562
-
-
Veazey, R.S.1
Klasse, P.J.2
Ketas, T.J.3
Reeves, J.D.4
Piatak Jr., M.5
Kunstman, K.6
Kuhmann, S.E.7
Marx, P.A.8
Lifson, J.D.9
Dufour, J.10
Mefford, M.11
Pandrea, I.12
Wolinsky, S.M.13
Doms, R.W.14
Demartino, J.A.15
Siciliano, S.J.16
Lyons, K.17
Springer, M.S.18
Moore, J.P.19
-
42
-
-
0028257964
-
Inhibition of human immunodeficiency virus infection by agents that interfere with thiol-disulfide interchange upon virus-receptor interaction
-
Ryser, H. J.-P.; Levy, E. M.; Mandel, R.; DiSciullo, G. J. Inhibition of human immunodeficiency virus infection by agents that interfere with thiol-disulfide interchange upon virus-receptor interaction. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4559-4563.
-
(1994)
Proc. Natl. Acad. Sci. U.S.A.
, vol.91
, pp. 4559-4563
-
-
Ryser, H.J.-P.1
Levy, E.M.2
Mandel, R.3
Disciullo, G.J.4
-
43
-
-
0035282999
-
The catalytic activity of protein disulfide isomerase is involved in human immunodeficiency virus envelope-mediated membrane fusion after CD4 cell binding
-
Fenouillet, E.; Barbouche, R.; Courageot, J.; Miquelis, R. The catalytic activity of protein disulfide isomerase is involved in human immunodeficiency virus envelope-mediated membrane fusion after CD4 cell binding. J. Infect. Dis. 2001, 183, 744-752.
-
(2001)
J. Infect. Dis.
, vol.183
, pp. 744-752
-
-
Fenouillet, E.1
Barbouche, R.2
Courageot, J.3
Miquelis, R.4
-
44
-
-
0345772126
-
Inhibitors of protein-disulfide isomerase prevent cleavage of disulfide bonds in receptor-bound glycoprotein 120 and prevent HIV-1 entry
-
Gallina, A.; Hanley, T. M.; Mandel, R.; Trahey, M.; Broder, C. C.; Viglianti, G. A.; Ryser, H. J. Inhibitors of protein-disulfide isomerase prevent cleavage of disulfide bonds in receptor-bound glycoprotein 120 and prevent HIV-1 entry. J. Biol. Chem. 2002, 277, 50579-50588.
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 50579-50588
-
-
Gallina, A.1
Hanley, T.M.2
Mandel, R.3
Trahey, M.4
Broder, C.C.5
Viglianti, G.A.6
Ryser, H.J.7
-
45
-
-
0037474328
-
Protein-disulfide isomerase-mediated reduction of two disulfide bonds of HIV envelope glycoprotein 120 occurs post-CXCR4 binding and is required for fusion
-
Barbouche, R.; Miquelis, R.; Jones, I. M.; Fenouillet, E. Protein-disulfide isomerase-mediated reduction of two disulfide bonds of HIV envelope glycoprotein 120 occurs post-CXCR4 binding and is required for fusion. J. Biol. Chem. 2003, 278, 3131-3136.
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 3131-3136
-
-
Barbouche, R.1
Miquelis, R.2
Jones, I.M.3
Fenouillet, E.4
-
46
-
-
0031729823
-
Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entry
-
Kilby, J. M.; Hopkins, S.; Venetta, S. M.; DiMassimo, B.; Cloud, G. A.; Lee, J. Y.; Alldredge, L.; Hunter, E.; Lambert, D.; Bolognesi, D.; Matthews, T.; Johnson, M. R.; Nowak, M. A.; Shaw, G. M.; Saag, M. S. Potent suppression of HIV-1 replication in humans by T-20, a peptide inhibitor of gp41-mediated virus entry. Nat. Med. 1998, 4, 1302-1307.
-
(1998)
Nat. Med.
, vol.4
, pp. 1302-1307
-
-
Kilby, J.M.1
Hopkins, S.2
Venetta, S.M.3
Dimassimo, B.4
Cloud, G.A.5
Lee, J.Y.6
Alldredge, L.7
Hunter, E.8
Lambert, D.9
Bolognesi, D.10
Matthews, T.11
Johnson, M.R.12
Nowak, M.A.13
Shaw, G.M.14
Saag, M.S.15
-
47
-
-
0038576281
-
Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America
-
Lalezari, J. P.; Henry, K.; O'Hearn, M.; Montaner, J. S. G.; Piliero, P. J.; Trottier, B.; Walmsley, S.; Cohen, C.; Kuritzkes, D. R.; Eron, J. J., Jr.; Chung, J.; DeMasi, R.; Donatacci, L.; Drobnes, C.; Delehanty, J.; Salgo, M. Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. N. Engl. J. Med. 2003, 348, 2175-2185.
-
(2003)
N. Engl. J. Med.
, vol.348
, pp. 2175-2185
-
-
Lalezari, J.P.1
Henry, K.2
O'Hearn, M.3
Montaner, J.S.G.4
Piliero, P.J.5
Trottier, B.6
Walmsley, S.7
Cohen, C.8
Kuritzkes, D.R.9
Eron Jr., J.J.10
Chung, J.11
Demasi, R.12
Donatacci, L.13
Drobnes, C.14
Delehanty, J.15
Salgo, M.16
-
48
-
-
0037849954
-
Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia
-
Lazzarin, A.; Clotet, B.; Cooper, D.; Reynes, J.; Arastéh, K.; Nelson, M.; Katlama, C.; Stellbrink, H.-J.; Delfraissy, J.-F.; Lange, J.; Huson, L.; DeMasi, R.; Wat, C.; Delehanty, J.; Drobnes, C.; Salgo, M. Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. N. Engl. J. Med. 2003, 348, 2186-2195.
-
(2003)
N. Engl. J. Med.
, vol.348
, pp. 2186-2195
-
-
Lazzarin, A.1
Clotet, B.2
Cooper, D.3
Reynes, J.4
Arastéh, K.5
Nelson, M.6
Katlama, C.7
Stellbrink, H.-J.8
Delfraissy, J.-F.9
Lange, J.10
Huson, L.11
Demasi, R.12
Wat, C.13
Delehanty, J.14
Drobnes, C.15
Salgo, M.16
-
49
-
-
0242705329
-
Enfuvirtide TORO studies: 48 week results confirm 24 week findings
-
Paris, France, July 14-17
-
Katlama, C.; Arastéh, K.; Clotet, B.; Cooper, D.; Henry, K.; Lalezari, J.; Lazzarin, A.; Montaner, J.; Nelson, M.; O'Hearn, M.; Piliero, P.; Reynes, J.; Trottier, B.; Walmsley, S.; DeMasi, R.; Delehanty, J.; Chung, J.; Salgo, M. Enfuvirtide TORO studies: 48 week results confirm 24 week findings. Presented at the 2nd IAS Conference on HIV and Pathogenesis, Paris, France, July 14-17, 2003.
-
(2003)
2nd IAS Conference on HIV and Pathogenesis
-
-
Katlama, C.1
Arastéh, K.2
Clotet, B.3
Cooper, D.4
Henry, K.5
Lalezari, J.6
Lazzarin, A.7
Montaner, J.8
Nelson, M.9
O'Hearn, M.10
Piliero, P.11
Reynes, J.12
Trottier, B.13
Walmsley, S.14
Demasi, R.15
Delehanty, J.16
Chung, J.17
Salgo, M.18
-
50
-
-
1642357851
-
Analysis of virological response of enfuvirtide in TORO: Implications for patient management
-
Paris, France, July 14-17
-
Montaner, J.; DeMasi, R.; Delehanty, J.; Chung, J.; Gafoor, Z.; Salgo, M. Analysis of virological response of enfuvirtide in TORO: implications for patient management. Presented at the 2nd IAS Conference on HIV and Pathogenesis, Paris, France, July 14-17, 2003.
-
(2003)
2nd IAS Conference on HIV and Pathogenesis
-
-
Montaner, J.1
Demasi, R.2
Delehanty, J.3
Chung, J.4
Gafoor, Z.5
Salgo, M.6
-
51
-
-
0037667047
-
Large-scale manufacture of peptide therapeutics by chemical synthesis
-
Bray, B. L. Large-scale manufacture of peptide therapeutics by chemical synthesis. Nat. Rev. Drug Discovery 2003, 2, 587-593.
-
(2003)
Nat. Rev. Drug Discovery
, vol.2
, pp. 587-593
-
-
Bray, B.L.1
-
52
-
-
0031883832
-
Determinants of human immunodeficiency virus type 1 resistance to gp41-derived inhibitory peptides
-
Rimsky, L. T.; Shugars, D. C.; Matthews, T. J. Determinants of human immunodeficiency virus type 1 resistance to gp41-derived inhibitory peptides. J. Virol. 1998, 72, 986-993.
-
(1998)
J. Virol.
, vol.72
, pp. 986-993
-
-
Rimsky, L.T.1
Shugars, D.C.2
Matthews, T.J.3
-
53
-
-
0036090585
-
Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy
-
Wei, X.; Decker, J. M.; Liu, H.; Zhang, Z.; Arani, R. B.; Kilby, J. M.; Saag, M. S.; Wu, X.; Shaw, G. M.; Kappes, J. C. Emergence of resistant human immunodeficiency virus type 1 in patients receiving fusion inhibitor (T-20) monotherapy. Antimicrob. Agents Chemother. 2002, 46, 1896-1905.
-
(2002)
Antimicrob. Agents Chemother.
, vol.46
, pp. 1896-1905
-
-
Wei, X.1
Decker, J.M.2
Liu, H.3
Zhang, Z.4
Arani, R.B.5
Kilby, J.M.6
Saag, M.S.7
Wu, X.8
Shaw, G.M.9
Kappes, J.C.10
-
54
-
-
1542372469
-
Analysis of patient-derived HIV-1 isolates suggests a novel mechanism for decreased sensitivity to inhibition by enfuvirtide and T-649
-
Boston, MA, February 10-14; Abstract 615
-
th Conference on Retroviruses and Opportunistic Infections, Boston, MA, February 10-14, 2003; Abstract 615.
-
(2003)
th Conference on Retroviruses and Opportunistic Infections
-
-
Heil, M.1
Decker, J.2
Chen, D.-T.3
Sfakianos, J.4
Shaw, G.5
Hunter, E.6
Derdeyn, C.7
-
55
-
-
0345700287
-
Entry inhibitors SCH-C, RANTES, and T-20 block HIV type 1 replication in multiple cell types
-
Ketas, T. J.; Klasse, P. J.; Spenlehauer, C.; Nesin, M.; Frank, I.; Pope, M.; Strizki, J. M.; Reyes, G. R.; Baroudy, B. M.; Moore, J. P. Entry inhibitors SCH-C, RANTES, and T-20 block HIV type 1 replication in multiple cell types. AIDS Res. Hum. Retroviruses 2003, 19, 177-186.
-
(2003)
AIDS Res. Hum. Retroviruses
, vol.19
, pp. 177-186
-
-
Ketas, T.J.1
Klasse, P.J.2
Spenlehauer, C.3
Nesin, M.4
Frank, I.5
Pope, M.6
Strizki, J.M.7
Reyes, G.R.8
Baroudy, B.M.9
Moore, J.P.10
-
56
-
-
0034801374
-
Toward proteomimetics: Terphenyl derivatives as structural and functional mimics of extended regions of an α-helix
-
Orner, B. P.; Ernst, J. T.; Hamilton, A. D. Toward proteomimetics: terphenyl derivatives as structural and functional mimics of extended regions of an α-helix. J. Am. Chem. Soc. 2001, 123, 5382-5383.
-
(2001)
J. Am. Chem. Soc.
, vol.123
, pp. 5382-5383
-
-
Orner, B.P.1
Ernst, J.T.2
Hamilton, A.D.3
-
57
-
-
0037126834
-
Design of a protein surface antagonist based on α-helix mimicry: Inhibition of gp41 assembly and viral fusion
-
Ernst, J. T.; Kutzki, O.; Debnath, A. K.; Jiang, S.; Lu, H.; Hamilton, A. D. Design of a protein surface antagonist based on α-helix mimicry: inhibition of gp41 assembly and viral fusion. Angew. Chem., Int. Ed. 2002, 41, 278-281.
-
(2002)
Angew. Chem., Int. Ed.
, vol.41
, pp. 278-281
-
-
Ernst, J.T.1
Kutzki, O.2
Debnath, A.K.3
Jiang, S.4
Lu, H.5
Hamilton, A.D.6
-
58
-
-
0037069386
-
Short constrained peptides that inhibit HIV-1 entry
-
Sia, S. K.; Carr, P. A.; Cochran, A. G.; Malashkevich, V. N.; Kim, P. S. Short constrained peptides that inhibit HIV-1 entry. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 14664-14669.
-
(2002)
Proc. Natl. Acad. Sci. U.S.A.
, vol.99
, pp. 14664-14669
-
-
Sia, S.K.1
Carr, P.A.2
Cochran, A.G.3
Malashkevich, V.N.4
Kim, P.S.5
-
59
-
-
0034752631
-
Prototype trial design for rapid dose selection of antiretroviral drugs: An example using emtricitabine (Coviracil)
-
Rousseau, F. S.; Kahn, J. O.; Thompson, M.; Mildvan, D.; Shepp, D.; Sommadossi, J. P.; Delehanty, J.; Simpson, J. N.; Wang, L. H.; Quinn, J. B.; Wakeford, C.; van der Horst, C. Prototype trial design for rapid dose selection of antiretroviral drugs: an example using emtricitabine (Coviracil). J. Antimicrob. Chemother. 2001, 48, 507-513.
-
(2001)
J. Antimicrob. Chemother.
, vol.48
, pp. 507-513
-
-
Rousseau, F.S.1
Kahn, J.O.2
Thompson, M.3
Mildvan, D.4
Shepp, D.5
Sommadossi, J.P.6
Delehanty, J.7
Simpson, J.N.8
Wang, L.H.9
Quinn, J.B.10
Wakeford, C.11
Van Der Horst, C.12
-
60
-
-
0033847883
-
Once-daily combination therapy with emtricitabine, didanosine, and efavirenz in human immunodeficiency virus-infected patients
-
Molina, J. M.; Ferchal, F.; Rancinan, C.; Raffi, F.; Rozenbaum, W.; Sereni, D.; Morlat, P.; Journot, V.; Decazes, J. M.; Chene, G. Once-daily combination therapy with emtricitabine, didanosine, and efavirenz in human immunodeficiency virus-infected patients. J. Infect. Dis. 2000, 182, 599-602.
-
(2000)
J. Infect. Dis.
, vol.182
, pp. 599-602
-
-
Molina, J.M.1
Ferchal, F.2
Rancinan, C.3
Raffi, F.4
Rozenbaum, W.5
Sereni, D.6
Morlat, P.7
Journot, V.8
Decazes, J.M.9
Chene, G.10
-
61
-
-
1642495257
-
A randomized, double-blind, multicenter comparison of emtricitabine QD to stavudine BID in treatment-naive HIV-infected patients
-
Paris, France, July 14-17
-
Raffi, F.; Saag, M.; Cahn, P.; Wolff, M.; Pearce, D.; Molina, J.; Hinkle, J.; Shaw, A.; Mondou, E.; Quinn, J.; Rousseau, F. A randomized, double-blind, multicenter comparison of emtricitabine QD to stavudine BID in treatment-naive HIV-infected patients. Presented at the 2nd IAS Conference on HIV and Pathogenesis, Paris, France, July 14-17, 2003.
-
(2003)
2nd IAS Conference on HIV and Pathogenesis
-
-
Raffi, F.1
Saag, M.2
Cahn, P.3
Wolff, M.4
Pearce, D.5
Molina, J.6
Hinkle, J.7
Shaw, A.8
Mondou, E.9
Quinn, J.10
Rousseau, F.11
-
62
-
-
0034944610
-
Antiretroviral activity of emtricitabine, a potent nucleoside reverse transcriptase inhibitor
-
Richman, D. D. Antiretroviral activity of emtricitabine, a potent nucleoside reverse transcriptase inhibitor. Antiviral Ther. 2001, 6, 83-88.
-
(2001)
Antiviral Ther.
, vol.6
, pp. 83-88
-
-
Richman, D.D.1
-
63
-
-
0037340618
-
Relative anti-HIV-1 efficacy of lamivudine and emtricitabine in vitro is dependent on cell type
-
Hazen, R.; Lanier, E. R. Relative anti-HIV-1 efficacy of lamivudine and emtricitabine in vitro is dependent on cell type. J. Acquired Immune Defic. Syndr. 2003, 32, 255-258.
-
(2003)
J. Acquired Immune Defic. Syndr.
, vol.32
, pp. 255-258
-
-
Hazen, R.1
Lanier, E.R.2
-
64
-
-
0033998526
-
Antiviral activity of 2′-deoxy-3′-oxa-4′-thiocytidine (BCH-10652) against lamivudine-resistant human immunodeficiency virus type 1 in SCID-hu Thy/Liv mice
-
(a) Stoddart, C. A.; Moreno, M. E.; Linquist-Stepps, V. D.; Bare, C.; Bogan, M. R.; Gobbi, A.; Buckheit, R. W., Jr.; Bedard, J.; Rando, R. F.; McCune, J. M. Antiviral activity of 2′-deoxy-3′-oxa-4′-thiocytidine (BCH-10652) against lamivudine-resistant human immunodeficiency virus type 1 in SCID-hu Thy/Liv mice. Antimicrob. Agents Chemother. 2000, 44, 783-786.
-
(2000)
Antimicrob. Agents Chemother.
, vol.44
, pp. 783-786
-
-
Stoddart, C.A.1
Moreno, M.E.2
Linquist-Stepps, V.D.3
Bare, C.4
Bogan, M.R.5
Gobbi, A.6
Buckheit Jr., R.W.7
Bedard, J.8
Rando, R.F.9
McCune, J.M.10
-
65
-
-
14944338926
-
Single and multiple dose pharmacokinetics and safety of the nucleoside Racivir in male volunteers
-
Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 044
-
(b) Otto, M. J.; Arastèh, K.; Schulbin, H.; Beard, A.; Cartee, L.; Liotta, D. C.; Schinazi, R. F.; Murphy, R. L. Single and multiple dose pharmacokinetics and safety of the nucleoside Racivir in male volunteers. Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 044; Antiviral Res. 2002, 51.
-
(2002)
Antiviral Res.
, pp. 51
-
-
Otto, M.J.1
Arastèh, K.2
Schulbin, H.3
Beard, A.4
Cartee, L.5
Liotta, D.C.6
Schinazi, R.F.7
Murphy, R.L.8
-
66
-
-
0029063384
-
Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2′-deoxy-3′-oxa-4′- thiocytidine and their 5-fluoro analogues in vitro
-
Mansour, T. S.; Jin, H.; Wang, W.; Hooker, E. U.; Ashman, C.; Cammack, N.; Salomon, H.; Belmonte, A. R.; Wainberg, M. A. Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2′-deoxy-3′-oxa-4′-thiocytidine and their 5-fluoro analogues in vitro. J. Med. Chem. 1995, 38, 1-4.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 1-4
-
-
Mansour, T.S.1
Jin, H.2
Wang, W.3
Hooker, E.U.4
Ashman, C.5
Cammack, N.6
Salomon, H.7
Belmonte, A.R.8
Wainberg, M.A.9
-
67
-
-
14944373457
-
Pharmacological evaluation of SPD754, a new NRTI
-
Toulon, France, June 3-5; Abstract OP 4.8
-
Bethell, R. Pharmacological evaluation of SPD754, a new NRTI. Presented at the 13th International Symposium on HIV & Emerging Infectious Diseases, Toulon, France, June 3-5, 2004; Abstract OP 4.8, p 60.
-
(2004)
13th International Symposium on HIV & Emerging Infectious Diseases
, pp. 60
-
-
Bethell, R.1
-
68
-
-
0023026496
-
Potent and selective anti-HTLV-III/LAV activity of 2′,3′- dideoxycytidinene, the 2′,3′-unsaturated derivative of 2′,3′-dideoxycytidine
-
Balzarini, J.; Pauwels, R.; Herdewijn, P.; De Clercq, E.; Cooney, D. A.; Kang, G. J.; Dalal, M.; Johns, D. G.; Broder, S. Potent and selective anti-HTLV-III/LAV activity of 2′,3′-dideoxycytidinene, the 2′,3′-unsaturated derivative of 2′,3′-dideoxycytidine. Biochem. Biophys. Res. Commun. 1988, 140, 735-742.
-
(1988)
Biochem. Biophys. Res. Commun.
, vol.140
, pp. 735-742
-
-
Balzarini, J.1
Pauwels, R.2
Herdewijn, P.3
De Clercq, E.4
Cooney, D.A.5
Kang, G.J.6
Dalal, M.7
Johns, D.G.8
Broder, S.9
-
69
-
-
0036232997
-
DPC 817: A cytidine nucleoside analog with activity against zidovudine- and lamivudine-resistant viral variants
-
Schinazi, R. F.; Mellors, J.; Bazmi, H.; Diamond, S.; Garber, S.; Gallagher, K.; Geleziunas, R.; Klabe, R.; Pierce, M.; Rayner, M.; Wu, J. T.; Zhang, H.; Hammond, J.; Bacheler, J.; Manion, D. J.; Otto, M. J.; Stuyver, L.; Trainor, G.; Liotta, D. C.; Erickson-Viitanen, S. DPC 817: a cytidine nucleoside analog with activity against zidovudine- and lamivudine-resistant viral variants. Antimicrob. Agents Chemother. 2002, 46, 1394-1401.
-
(2002)
Antimicrob. Agents Chemother.
, vol.46
, pp. 1394-1401
-
-
Schinazi, R.F.1
Mellors, J.2
Bazmi, H.3
Diamond, S.4
Garber, S.5
Gallagher, K.6
Geleziunas, R.7
Klabe, R.8
Pierce, M.9
Rayner, M.10
Wu, J.T.11
Zhang, H.12
Hammond, J.13
Bacheler, J.14
Manion, D.J.15
Otto, M.J.16
Stuyver, L.17
Trainor, G.18
Liotta, D.C.19
Erickson-Viitanen, S.20
more..
-
70
-
-
12444325183
-
HIV-1 resistance profile of the novel nucleoside reverse transcriptase inhibitor β-D-2′,3′-dideoxy-2′,3′-didehydro-5- fluorocytidine (Reverset)
-
Geleziunas, R.; Gallagher, K.; Zhang, H.; Bacheler, L.; Garber, S.; Wu, J.-T.; Shi, G.; Otto, M. J.; Schinazi, R. F.; Erickson-Viitanen, S. HIV-1 resistance profile of the novel nucleoside reverse transcriptase inhibitor β-D-2′,3′-dideoxy-2′,3′-didehydro-5-fluorocytidine (Reverset). Antiviral Chem. Chemother. 2003, 14, 49-59.
-
(2003)
Antiviral Chem. Chemother.
, vol.14
, pp. 49-59
-
-
Geleziunas, R.1
Gallagher, K.2
Zhang, H.3
Bacheler, L.4
Garber, S.5
Wu, J.-T.6
Shi, G.7
Otto, M.J.8
Schinazi, R.F.9
Erickson-Viitanen, S.10
-
71
-
-
12444267896
-
Cellular pharmacology of D-d4FC, a nucleoside analogue active against drug-resistant HIV
-
Erickson-Viitanen, S.; Wu, J.-T.; Shi, G.; Unger, S.; King, R. W.; Fish, B.; Klabe, R.; Geleziunas, R.; Gallagher, K.; Otto, M. J.; Schinazi, R. F. Cellular pharmacology of D-d4FC, a nucleoside analogue active against drug-resistant HIV. Antiviral Chem. Chemother. 2003, 14, 39-47.
-
(2003)
Antiviral Chem. Chemother.
, vol.14
, pp. 39-47
-
-
Erickson-Viitanen, S.1
Wu, J.-T.2
Shi, G.3
Unger, S.4
King, R.W.5
Fish, B.6
Klabe, R.7
Geleziunas, R.8
Gallagher, K.9
Otto, M.J.10
Schinazi, R.F.11
-
72
-
-
20144376405
-
Pharmacokinetics and safety of the nucleoside reverset in HIV-1 infected patients
-
Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 074
-
Murphy, R. L.; Schürmann, D.; Kravec, I.; Eron, J.; Havlir, D.; Beard, A.; Cartee, L.; Hurwitz, S. J.; Erickson-Viitanen, S; Liotta, D. C.; Schinazi, R. F.; Otto, M. J. Pharmacokinetics and safety of the nucleoside reverset in HIV-1 infected patients. Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 074; Antiviral Res. 2002, 86.
-
(2002)
Antiviral Res.
, pp. 86
-
-
Murphy, R.L.1
Schürmann, D.2
Kravec, I.3
Eron, J.4
Havlir, D.5
Beard, A.6
Cartee, L.7
Hurwitz, S.J.8
Erickson-Viitanen, S.9
Liotta, D.C.10
Schinazi, R.F.11
Otto, M.J.12
-
73
-
-
14944352550
-
Activity of the cytidine analog reverset (RVT) against 3TC-resistant HIV-1 in SCID-hu Thy/Liv mice
-
Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 023
-
Stoddart, C. A.; Bozeman, C. A.; Schinazi, R. F. Activity of the cytidine analog reverset (RVT) against 3TC-resistant HIV-1 in SCID-hu Thy/Liv mice. Presented at HIV DART 2002, Frontiers in Drug Development for Antiretroviral Therapies, Naples, FL, December 15-19, 2002; Abstract 023; Antiviral Res. 2002, 29.
-
(2002)
Antiviral Res.
, pp. 29
-
-
Stoddart, C.A.1
Bozeman, C.A.2
Schinazi, R.F.3
-
74
-
-
0035162759
-
Mechanism of action of 1-β-D-2,6-diaminopurine dioxolane, a prodrug of the human immunodeficiency virus type 1 inhibitor 1-β-D-dioxolane guanosine
-
Furman, P. A.; Jeffrey, J.; Kiefer, L. L.; Feng, J. Y.; Anderson, K. S.; Borroto-Esoda, K.; Hill, E.; Copeland, W. C.; Chu, C. K.; Sommadossi, J. P.; Liberman, L; Schinazi, R. F.; Painter, G. R. Mechanism of action of 1-β-D-2,6-diaminopurine dioxolane, a prodrug of the human immunodeficiency virus type 1 inhibitor 1-β-D-dioxolane guanosine. Antimicrob. Agents Chemother. 2001, 45, 158-165.
-
(2001)
Antimicrob. Agents Chemother.
, vol.45
, pp. 158-165
-
-
Furman, P.A.1
Jeffrey, J.2
Kiefer, L.L.3
Feng, J.Y.4
Anderson, K.S.5
Borroto-Esoda, K.6
Hill, E.7
Copeland, W.C.8
Chu, C.K.9
Sommadossi, J.P.10
Liberman, L.11
Schinazi, R.F.12
Painter, G.R.13
-
75
-
-
0038143190
-
Dioxolane guanosine 5′-triphosphate, an alternative substrate inhibitor of wild-type and mutant HIV-1 reverse transcriptase
-
Jeffrey, J. L.; Feng, J. Y.; Qi, C. C. R.; Anderson, K. S.; Furman, P. A. Dioxolane guanosine 5′-triphosphate, an alternative substrate inhibitor of wild-type and mutant HIV-1 reverse transcriptase. J. Biol. Chem. 2003, 278, 18971-18979.
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 18971-18979
-
-
Jeffrey, J.L.1
Feng, J.Y.2
Qi, C.C.R.3
Anderson, K.S.4
Furman, P.A.5
-
76
-
-
12244301646
-
Enzymatic assay for measurement of intracellular DXG triphosphate concentrations in peripheral blood mononuclear cells from human immunodeficiency virus type 1-infected patients
-
Kewn, S.; Wang, L. H.; Hoggard, P. G.; Rousseau, F.; Hart, R.; MacNeela, J. P.; Khoo, S. H.; Back, D. J. Enzymatic assay for measurement of intracellular DXG triphosphate concentrations in peripheral blood mononuclear cells from human immunodeficiency virus type 1-infected patients. Antimicrob. Agents Chemother. 2003, 47, 255-261.
-
(2003)
Antimicrob. Agents Chemother.
, vol.47
, pp. 255-261
-
-
Kewn, S.1
Wang, L.H.2
Hoggard, P.G.3
Rousseau, F.4
Hart, R.5
MacNeela, J.P.6
Khoo, S.H.7
Back, D.J.8
-
77
-
-
0011263710
-
Anabolic profile of the dioxolane nucleoside analogue DXG in human PBMC; reversal of resistance by boosting 5′-triphosphate levels
-
Presented at the 15th International Conference on Antiviral Research, Prague, Czech Republic, March 17-21, 2002; Abstract A37, No. 7
-
Painter, G. R.; St Claire, R.; Feng, J.; Borroto-Esoda, K. Anabolic profile of the dioxolane nucleoside analogue DXG in human PBMC; reversal of resistance by boosting 5′-triphosphate levels. Presented at the 15th International Conference on Antiviral Research, Prague, Czech Republic, March 17-21, 2002; Abstract A37, No. 7; Antiviral Res. 2002, 53, A37.
-
(2002)
Antiviral Res.
, vol.53
-
-
Painter, G.R.1
St. Claire, R.2
Feng, J.3
Borroto-Esoda, K.4
-
78
-
-
0036156325
-
Dioxolane guanosine, the active form of the prodrug diaminopurine dioxolane, is a potent inhibitor of drug-resistant HIV-1 isolates from patients for whom standard nucleoside therapy fails
-
Mewshaw, J. P.; Myrick, F. T.; Wakefield, D. A. C. S.; Hooper, B. J.; Harris, J. L.; McCreedy, B.; Borroto-Esoda, K. Dioxolane guanosine, the active form of the prodrug diaminopurine dioxolane, is a potent inhibitor of drug-resistant HIV-1 isolates from patients for whom standard nucleoside therapy fails. J. Acquired Immune Defic. Syndr. 2002, 29, 11-20.
-
(2002)
J. Acquired Immune Defic. Syndr.
, vol.29
, pp. 11-20
-
-
Mewshaw, J.P.1
Myrick, F.T.2
Wakefield, D.A.C.S.3
Hooper, B.J.4
Harris, J.L.5
McCreedy, B.6
Borroto-Esoda, K.7
-
79
-
-
2342451795
-
Potential of acyclic nucleoside phosphonates in the treatment of DNA virus and retrovirus infections
-
De Clercq, E. Potential of acyclic nucleoside phosphonates in the treatment of DNA virus and retrovirus infections. Expert Rev. Anti-Infect. Ther. 2003, 1, 21-43.
-
(2003)
Expert Rev. Anti-Infect. Ther.
, vol.1
, pp. 21-43
-
-
De Clercq, E.1
-
80
-
-
0038372726
-
Extended treatment with tenofovir disoproxil fumarate in treatment-experienced HIV-1-infected patients: Genotypic, phenotypic, and rebound analyses
-
Margot, N. A.; Isaacson, E.; McGowan, I.; Cheng, A.; Miller, M. D. Extended treatment with tenofovir disoproxil fumarate in treatment-experienced HIV-1-infected patients: genotypic, phenotypic, and rebound analyses. J. Acquired Immune Defic. Syndr. 2003, 33, 15-21.
-
(2003)
J. Acquired Immune Defic. Syndr.
, vol.33
, pp. 15-21
-
-
Margot, N.A.1
Isaacson, E.2
McGowan, I.3
Cheng, A.4
Miller, M.D.5
-
81
-
-
0003289087
-
Efficacy and safety of tenofovir disoproxil fumarate (TDF) versus stavudine (d4T) when used in combination with lamivudine (3TC) and efavirenz (EFV) in HIV-1 infected patients naive to antiretroviral therapy (ART): 48-Week interim results
-
Barcelona, Spain, July 7-12; Abstract Or17
-
Staszewski, S.; Gallant, J.; Pozniak, A.; Suleiman, J. M. A. H.; Dejesus, E.; Koenig, E.; Coleman, S.; Lu, B.; Cheng, A. K.; Coakley, D. F. Efficacy and safety of tenofovir disoproxil fumarate (TDF) versus stavudine (d4T) when used in combination with lamivudine (3TC) and efavirenz (EFV) in HIV-1 infected patients naive to antiretroviral therapy (ART): 48-week interim results. Presented at the XIV International AIDS Conference, Barcelona, Spain, July 7-12, 2002; Abstract Or17.
-
(2002)
XIV International AIDS Conference
-
-
Staszewski, S.1
Gallant, J.2
Pozniak, A.3
Suleiman, J.M.A.H.4
Dejesus, E.5
Koenig, E.6
Coleman, S.7
Lu, B.8
Cheng, A.K.9
Coakley, D.F.10
-
82
-
-
0012774175
-
Efficacy and safety of tenofovir DF (TDF) versus stavudine (d4T) when used in combination with lamivudine and efavirenz in antiretroviral naive patients: 96-Week preliminary interim results
-
Boston, MA, February 10-14; Abstract 564b
-
Staszewski, S.; Gallant, J. E.; Pozniak, A. L.; Suleiman, J. M. A. H.; DeJesus, E.; Lu, B.; Sayre, J.; Cheng, A. Efficacy and safety of tenofovir DF (TDF) versus stavudine (d4T) when used in combination with lamivudine and efavirenz in antiretroviral naive patients: 96-week preliminary interim results. Presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA, February 10-14, 2003; Abstract 564b.
-
(2003)
10th Conference on Retroviruses and Opportunistic Infections
-
-
Staszewski, S.1
Gallant, J.E.2
Pozniak, A.L.3
Suleiman, J.M.A.H.4
Dejesus, E.5
Lu, B.6
Sayre, J.7
Cheng, A.8
-
83
-
-
14944385086
-
New antiretrovirals and strategies in the Gilead pipeline
-
Toulon, France, June 3-5; Abstract OP 4.3
-
Rooney, J. F.; Cheng, A.; Lee, W. A. New antiretrovirals and strategies in the Gilead pipeline. Presented at the 13th International Symposium on HIV & Emerging Infectious Diseases, Toulon, France, June 3-5, 2004; Abstract OP 4.3, p 55.
-
(2004)
13th International Symposium on HIV & Emerging Infectious Diseases
, pp. 55
-
-
Rooney, J.F.1
Cheng, A.2
Lee, W.A.3
-
84
-
-
0037111084
-
Topical administration of low-dose tenofovir disoproxil fumarate to protect infant macaques against multiple oral exposures of low doses of simian immunodeficiency virus
-
Van Rompay, K. K. A.; Schmidt, K. A.; Lawson, J. R.; Singh, R.; Bischofberger, N.; Marthas, M. L. Topical administration of low-dose tenofovir disoproxil fumarate to protect infant macaques against multiple oral exposures of low doses of simian immunodeficiency virus. J. Infect. Dis. 2002, 186, 1508-1513.
-
(2002)
J. Infect. Dis.
, vol.186
, pp. 1508-1513
-
-
Van Rompay, K.K.A.1
Schmidt, K.A.2
Lawson, J.R.3
Singh, R.4
Bischofberger, N.5
Marthas, M.L.6
-
85
-
-
0037530011
-
Determining the antiviral activity of tenofovir disoproxil fumarate in treatment-naive chronically HIV-1-infected individuals
-
Louie, M.; Hogan, C.; Hurley, A.; Simon, V.; Chung, C.; Padte, N.; Lamy, P.; Flaherty, J.; Coakley, D.; Di Mascio, M.; Perelson, A. S.; Markowitz, M. Determining the antiviral activity of tenofovir disoproxil fumarate in treatment-naive chronically HIV-1-infected individuals. AIDS 2003, 17, 1151-1156.
-
(2003)
AIDS
, vol.17
, pp. 1151-1156
-
-
Louie, M.1
Hogan, C.2
Hurley, A.3
Simon, V.4
Chung, C.5
Padte, N.6
Lamy, P.7
Flaherty, J.8
Coakley, D.9
Di Mascio, M.10
Perelson, A.S.11
Markowitz, M.12
-
86
-
-
0037159877
-
Activity of tenofovir on hepatitis B virus replication in HIV-co-infected patients failing or partially responding to lamivudine
-
Nunez, M.; Pérez-Olmeda, M.; Diaz, B.; Rios, P.; Gonzalez-Lahoz, J.; Soriano, V. Activity of tenofovir on hepatitis B virus replication in HIV-co-infected patients failing or partially responding to lamivudine. AIDS 2002, 16, 2352-2354.
-
(2002)
AIDS
, vol.16
, pp. 2352-2354
-
-
Nunez, M.1
Pérez-Olmeda, M.2
Diaz, B.3
Rios, P.4
Gonzalez-Lahoz, J.5
Soriano, V.6
-
87
-
-
0037115019
-
Tenofovir disoproxil fumarate therapy for chronic hepatitis B in human immunodeficiency virus/hepatitis B virus-coinfected individuals for whom interferon-α and lamivudine therapy have failed
-
Ristig, M. B.; Crippin, J.; Aberg, J. A.; Powderly, W. G.; Lisker-Melman, M.; Kessels, L.; Tebas, P. Tenofovir disoproxil fumarate therapy for chronic hepatitis B in human immunodeficiency virus/hepatitis B virus-coinfected individuals for whom interferon-α and lamivudine therapy have failed. J. Infect. Dis. 2002, 186, 1844-1847.
-
(2002)
J. Infect. Dis.
, vol.186
, pp. 1844-1847
-
-
Ristig, M.B.1
Crippin, J.2
Aberg, J.A.3
Powderly, W.G.4
Lisker-Melman, M.5
Kessels, L.6
Tebas, P.7
-
88
-
-
0037426728
-
Tenofovir disoproxil fumarate in patients with HIV and lamivudine-resistant hepatitis B virus
-
Benhamou, Y.; Tubiana, R.; Thibault, V. Tenofovir disoproxil fumarate in patients with HIV and lamivudine-resistant hepatitis B virus. N. Engl. J. Med. 2003, 348, 177-178.
-
(2003)
N. Engl. J. Med.
, vol.348
, pp. 177-178
-
-
Benhamou, Y.1
Tubiana, R.2
Thibault, V.3
-
89
-
-
0037308267
-
Tenofovir disoproxil fumarate exhibits strong antiviral effect in a patient with lamivudine-resistant severe hepatitis B reactivation
-
Van Bömmel, F.; Schernick, A.; Hopf, U.; Berg, T. Tenofovir disoproxil fumarate exhibits strong antiviral effect in a patient with lamivudine-resistant severe hepatitis B reactivation. Gastroenterology 2003, 124, 586-587.
-
(2003)
Gastroenterology
, vol.124
, pp. 586-587
-
-
Van Bömmel, F.1
Schernick, A.2
Hopf, U.3
Berg, T.4
-
90
-
-
11244317278
-
Long-term tenofovir treatment of lamivudine-resistant chronic hepatitis B in HIV co-infected patients
-
Boston, MA; February 10-14 ; Abstract 824
-
Marcelin, A. G.; Tubiana, R.; Benhamou, Y.; Katlama, C.; Calvez, V.; Thibault, V. Long-term tenofovir treatment of lamivudine-resistant chronic hepatitis B in HIV co-infected patients. Presented at the 10th Conference on Retroviruses and Opportunistic Infections, Boston, MA; February 10-14, 2003; Abstract 824.
-
(2003)
10th Conference on Retroviruses and Opportunistic Infections
-
-
Marcelin, A.G.1
Tubiana, R.2
Benhamou, Y.3
Katlama, C.4
Calvez, V.5
Thibault, V.6
-
91
-
-
0032437454
-
The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection
-
De Clercq, E. The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection. Antiviral Res. 1998, 38, 153-179.
-
(1998)
Antiviral Res.
, vol.38
, pp. 153-179
-
-
De Clercq, E.1
-
92
-
-
0033986850
-
Safety assessment, in vitro and in vivo, and pharmacokinetics of emivirine, a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1
-
Szczech, G. M.; Furman, P.; Painter, G. R.; Barry, D. W.; Borroto-Esoda, K.; Grizzle, T. B.; Blum, M. R.; Sommadossi, J.; Endoh, R.; Niwa, T.; Yamamoto, M.; Moxham, C. Safety assessment, in vitro and in vivo, and pharmacokinetics of emivirine, a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. Antimicrob. Agents Chemother. 2000, 44, 123-130.
-
(2000)
Antimicrob. Agents Chemother.
, vol.44
, pp. 123-130
-
-
Szczech, G.M.1
Furman, P.2
Painter, G.R.3
Barry, D.W.4
Borroto-Esoda, K.5
Grizzle, T.B.6
Blum, M.R.7
Sommadossi, J.8
Endoh, R.9
Niwa, T.10
Yamamoto, M.11
Moxham, C.12
-
93
-
-
0030997133
-
Chemical barriers to human immunodeficiency virus type 1 (HIV-1) infection: Retrovirucidal activity of UC781, a thiocarboxanilide nonnucleoside inhibitor of HIV-1 reverse transcriptase
-
Borkow, G.; Barnard, J.; Nguyen, T. M.; Belmonte, A.; Wainberg, M. A.; Parniak, M. A. Chemical barriers to human immunodeficiency virus type 1 (HIV-1) infection: retrovirucidal activity of UC781, a thiocarboxanilide nonnucleoside inhibitor of HIV-1 reverse transcriptase. J. Virol. 1997, 77, 3023-3030.
-
(1997)
J. Virol.
, vol.77
, pp. 3023-3030
-
-
Borkow, G.1
Barnard, J.2
Nguyen, T.M.3
Belmonte, A.4
Wainberg, M.A.5
Parniak, M.A.6
-
94
-
-
0032500021
-
Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent
-
Balzarini, J.; Naesens, L.; Verbeken, E.; Laga, M.; Van Damme, L.; Parniak, M.; Van Mellaert, L.; Anné, J.; De Clercq, E. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS 1998, 72, 1129-1138.
-
(1998)
AIDS
, vol.72
, pp. 1129-1138
-
-
Balzarini, J.1
Naesens, L.2
Verbeken, E.3
Laga, M.4
Van Damme, L.5
Parniak, M.6
Van Mellaert, L.7
Anné, J.8
De Clercq, E.9
-
95
-
-
0034640387
-
Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 reverse trancriptase involves extensive main chain hydrogen bonding
-
Ren, J.; Nichols, C.; Bird, L. E.; Fujiwara, T.; Sugimoto, H.; Stuart, D. L; Stammers, D. K. Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 reverse trancriptase involves extensive main chain hydrogen bonding. J. Biol. Chem. 2000, 275, 14316-14320.
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 14316-14320
-
-
Ren, J.1
Nichols, C.2
Bird, L.E.3
Fujiwara, T.4
Sugimoto, H.5
Stuart, D.L.6
Stammers, D.K.7
-
96
-
-
0032786364
-
Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1
-
Corbett, J. W.; Ko, S. S.; Rodgers, J. D.; Jeffrey, S.; Bacheler, L. T.; Klabe, R. M.; Diamond, S.; Lai, C. M.; Rabel, S. R.; Saye, J. A.; Adams, S. P.; Trainor, G. L.; Anderson, P. S.; Erickson-Viitanen, S. K. Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1. Antimicrob. Agents Chemother. 1999, 43, 2893-2897.
-
(1999)
Antimicrob. Agents Chemother.
, vol.43
, pp. 2893-2897
-
-
Corbett, J.W.1
Ko, S.S.2
Rodgers, J.D.3
Jeffrey, S.4
Bacheler, L.T.5
Klabe, R.M.6
Diamond, S.7
Lai, C.M.8
Rabel, S.R.9
Saye, J.A.10
Adams, S.P.11
Trainor, G.L.12
Anderson, P.S.13
Erickson-Viitanen, S.K.14
-
97
-
-
0034128898
-
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors
-
Corbett, J. W.; Ko, S. S.; Rodgers, J. D.; Gearhart, L. A.; Magnus, N. A.; Bacheler, L. T.; Diamond, S.; Jeffrey, S.; Klabe, R. M.; Cordova, B. C.; Garber, S.; Logue, K.; Trainor, G. L.; Anderson, P. S.; Erickson-Viitanen, S. K. Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors. J. Med. Chem. 2000, 43, 2019-2030.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 2019-2030
-
-
Corbett, J.W.1
Ko, S.S.2
Rodgers, J.D.3
Gearhart, L.A.4
Magnus, N.A.5
Bacheler, L.T.6
Diamond, S.7
Jeffrey, S.8
Klabe, R.M.9
Cordova, B.C.10
Garber, S.11
Logue, K.12
Trainor, G.L.13
Anderson, P.S.14
Erickson-Viitanen, S.K.15
-
98
-
-
0003259264
-
(The DPC 083-203 Study Team) Study of DPC 083-203, a phase II comparison of 100 and 200 mg once-daily DPC 083 and 2 NRTIs in patients failing a NNRTI-containing regimen
-
Seattle, WA; February 24-28; Abstract 6
-
Ruiz, N.; Nusrat, R.; Lauenroth-Mai, E.; Berger, D.; Walworth, C.; Bacheler, L. T.; Ploughman, L.; Tsang, P.; Labriola, D.; Echols, R.; Levy, R. (The DPC 083-203 Study Team) Study of DPC 083-203, a phase II comparison of 100 and 200 mg once-daily DPC 083 and 2 NRTIs in patients failing a NNRTI-containing regimen. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA; February 24-28, 2002; Abstract 6, p 55.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 55
-
-
Ruiz, N.1
Nusrat, R.2
Lauenroth-Mai, E.3
Berger, D.4
Walworth, C.5
Bacheler, L.T.6
Ploughman, L.7
Tsang, P.8
Labriola, D.9
Echols, R.10
Levy, R.11
-
99
-
-
0003259264
-
A phase II double-blind (DB) comparison of 3 once daily doses of the NNRTI DPC 083 vs 600 mg efavirenz (EFV) in combination with 2 NRTIs in HIV antiretroviral (ARV) treatment-naive patients
-
Seattle, WA, February 24-28; Abstract
-
Ruiz, N.; Nusrat, R.; Lazzarin, A.; Arasteh, K.; Goebel, F.-D.; Audagnotto, S.; Rachlis, A.; Arribas, J.; Ploughman, L.; Fiske, W.; Labriola, D.; Levy, R.; Echols, R. A phase II double-blind (DB) comparison of 3 once daily doses of the NNRTI DPC 083 vs 600 mg efavirenz (EFV) in combination with 2 NRTIs in HIV antiretroviral (ARV) treatment-naive patients. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002; Abstract 7, p 55.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, vol.7
, pp. 55
-
-
Ruiz, N.1
Nusrat, R.2
Lazzarin, A.3
Arasteh, K.4
Goebel, F.-D.5
Audagnotto, S.6
Rachlis, A.7
Arribas, J.8
Ploughman, L.9
Fiske, W.10
Labriola, D.11
Levy, R.12
Echols, R.13
-
100
-
-
0009505878
-
R165335-TMC125, a novel non nucleoside reverse transcriptase inhibitor (NNRTI) with nanomolar activity against NNRTI resistant HIV strains
-
Toronto, Canada, September 17-20 ; Abstract 1840
-
Andries, K., de Béthune, M.-P.; Kukla, M. J.; Azijn, H.; Lewi, P. J.; Janssen, P. A. J.; Pauwels, R. R165335-TMC125, a novel non nucleoside reverse transcriptase inhibitor (NNRTI) with nanomolar activity against NNRTI resistant HIV strains. Presented at the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy, Toronto, Canada, September 17-20, 2000; Abstract 1840.
-
(2000)
40th Interscience Conference on Antimicrobial Agents and Chemotherapy
-
-
Andries, K.1
De Béthune, M.-P.2
Kukla, M.J.3
Azijn, H.4
Lewi, P.J.5
Janssen, P.A.J.6
Pauwels, R.7
-
101
-
-
0011343037
-
TMC125, a next-generation NNRTI, demonstrates high potency after 7 days therapy in treatment-experienced HIV-1-infected individuals with phenotypic NNRTI resistance
-
Seattle, WA; February 24-28; Abstract 4
-
Gazzard, B.; Pozniak, A.; Arasteh, K.; Staszewski, S.; Rozenbaum, W.; Yeni, P.; van't Klooster, G.; De Dier, K.; Peeters, M.; de Béthune, M.-P.; Graham, N.; Pauwels, R. TMC125, a next-generation NNRTI, demonstrates high potency after 7 days therapy in treatment-experienced HIV-1-infected individuals with phenotypic NNRTI resistance. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA; February 24-28, 2002; Abstract 4, p 54.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 54
-
-
Gazzard, B.1
Pozniak, A.2
Arasteh, K.3
Staszewski, S.4
Rozenbaum, W.5
Yeni, P.6
Van't Klooster, G.7
De Dier, K.8
Peeters, M.9
De Béthune, M.-P.10
Graham, N.11
Pauwels, R.12
-
102
-
-
0037692641
-
TMC125 monotherapy for 1 week results in a similar initial rate of decline of HIV-1 RNA as therapy with a 5-drug regimen
-
Seattle, WA; February 24-28; Abstract 5
-
Sankatsing, S.; Weverling, G.; van't Klooster, G.; Prins, J.; Lange, J. TMC125 monotherapy for 1 week results in a similar initial rate of decline of HIV-1 RNA as therapy with a 5-drug regimen. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA; February 24-28, 2002; Abstract 5, p 54.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 54
-
-
Sankatsing, S.1
Weverling, G.2
Van't Klooster, G.3
Prins, J.4
Lange, J.5
-
103
-
-
12144287763
-
An open-label assessment of TMC 125, a new, next-generation NNRTI, for 7 days in HIV-1 infected individuals with NNRTI resistance
-
Gazzard, B. G.; Pozniak, A. L.; Rosenbaum, W.; Yeni, G. P.; Staszewski, S.; Arasteh, K.; De Dier, K.; Peeters, M.; Woodfall, B.; Stebbing, J.; van't Klooster, G. A. An open-label assessment of TMC 125, a new, next-generation NNRTI, for 7 days in HIV-1 infected individuals with NNRTI resistance. AIDS 2003, 17, F49-F54.
-
(2003)
AIDS
, vol.17
-
-
Gazzard, B.G.1
Pozniak, A.L.2
Rosenbaum, W.3
Yeni, G.P.4
Staszewski, S.5
Arasteh, K.6
De Dier, K.7
Peeters, M.8
Woodfall, B.9
Stebbing, J.10
Van't Klooster, G.A.11
-
104
-
-
0041488800
-
Small-molecule HIV-1 integrase inhibitors: The 2001-2002 update
-
Dayam, R.; Neamati, N. Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update. Curr. Pharm. Des. 2003, 9, 1789-1902.
-
(2003)
Curr. Pharm. Des.
, vol.9
, pp. 1789-1902
-
-
Dayam, R.1
Neamati, N.2
-
105
-
-
0031685017
-
Resistance to the anti-human immunodeficiency virus type 1 compound L-chicoric acid results from a single mutation at amino acid 140 of integrase
-
King, P. J.; Robinson, W. E., Jr. Resistance to the anti-human immunodeficiency virus type 1 compound L-chicoric acid results from a single mutation at amino acid 140 of integrase. J. Virol. 1998, 72, 8420-8424.
-
(1998)
J. Virol.
, vol.72
, pp. 8420-8424
-
-
King, P.J.1
Robinson Jr., W.E.2
-
106
-
-
0037293099
-
Human immunodeficiency virus type-1 integrase containing a glycine to serine mutation at position 140 is attenuated for catalysis and resistant to integrase inhibitors
-
King, P. J.; Lee, D. J.; Reinke, R. A.; Victoria, J. G.; Beale, K.; Robinson, W. E., Jr. Human immunodeficiency virus type-1 integrase containing a glycine to serine mutation at position 140 is attenuated for catalysis and resistant to integrase inhibitors. Virology 2003, 306, 147-161.
-
(2003)
Virology
, vol.306
, pp. 147-161
-
-
King, P.J.1
Lee, D.J.2
Reinke, R.A.3
Victoria, J.G.4
Beale, K.5
Robinson Jr., W.E.6
-
107
-
-
0033856959
-
Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters
-
Pluymers, W.; Neamati, N.; Pannecouque, C.; Fikkert, V.; Marchand, C.; Burke, T. R., Jr.; Pommier, Y.; Schols, D.; De Clercq, E.; Debyser, Z.; Witvrouw, M. Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters. Mol. Pharmacol. 2000, 58, 641-648.
-
(2000)
Mol. Pharmacol.
, vol.58
, pp. 641-648
-
-
Pluymers, W.1
Neamati, N.2
Pannecouque, C.3
Fikkert, V.4
Marchand, C.5
Burke Jr., T.R.6
Pommier, Y.7
Schols, D.8
De Clercq, E.9
Debyser, Z.10
Witvrouw, M.11
-
108
-
-
13044295993
-
Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: A platform for antiviral drug design
-
Goldgur, Y.; Craigie, R.; Cohen, G. H.; Fujiwara, T.; Yoshinaga, T.; Fujishita, T.; Sugimoto, H.; Endo, T.; Murai, H.; Davies, D. R. Structure of the HIV-1 integrase catalytic domain complexed with an inhibitor: a platform for antiviral drug design. Proc. Natl. Acad. Sci. U.S.A. 1999, 96, 13040-13043.
-
(1999)
Proc. Natl. Acad. Sci. U.S.A.
, vol.96
, pp. 13040-13043
-
-
Goldgur, Y.1
Craigie, R.2
Cohen, G.H.3
Fujiwara, T.4
Yoshinaga, T.5
Fujishita, T.6
Sugimoto, H.7
Endo, T.8
Murai, H.9
Davies, D.R.10
-
109
-
-
0034723439
-
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
-
Hazuda, D. J.; Felock, P.; Witmer, M.; Wolfe, A.; Stillmock, K.; Grobler, J. A.; Espeseth, A.; Gabryelski, L.; Schleif, W.; Blau, C.; Miller, M. D. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 2000, 287, 646-650.
-
(2000)
Science
, vol.287
, pp. 646-650
-
-
Hazuda, D.J.1
Felock, P.2
Witmer, M.3
Wolfe, A.4
Stillmock, K.5
Grobler, J.A.6
Espeseth, A.7
Gabryelski, L.8
Schleif, W.9
Blau, C.10
Miller, M.D.11
-
110
-
-
0036784324
-
Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives
-
Pluymers, W.; Pais, G.; Van Maele, B.; Pannecouque, C.; Fikkert, V.; Burke, T. R., Jr.; De Clercq, E.; Witvrouw, M.; Neamati, N.; Debyser, Z. Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives. Antimicrob. Agents Chemother. 2002, 46, 3292-3297.
-
(2002)
Antimicrob. Agents Chemother.
, vol.46
, pp. 3292-3297
-
-
Pluymers, W.1
Pais, G.2
Van Maele, B.3
Pannecouque, C.4
Fikkert, V.5
Burke Jr., T.R.6
De Clercq, E.7
Witvrouw, M.8
Neamati, N.9
Debyser, Z.10
-
111
-
-
10744226580
-
Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations
-
Fikkert, V.; Van Maele, B.; Vercammen, J.; Hantson, A.; Van Remoortel, B.; Michiels, M.; Gurnari, C.; Pannecouque, C.; De Maeyer, M.; Engelborghs, Y.; De Clercq, E.; Debyser, Z.; Witvrouw, M. Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations. J. Virol. 2003, 77, 11459-11470.
-
(2003)
J. Virol.
, vol.77
, pp. 11459-11470
-
-
Fikkert, V.1
Van Maele, B.2
Vercammen, J.3
Hantson, A.4
Van Remoortel, B.5
Michiels, M.6
Gurnari, C.7
Pannecouque, C.8
De Maeyer, M.9
Engelborghs, Y.10
De Clercq, E.11
Debyser, Z.12
Witvrouw, M.13
-
112
-
-
0003203586
-
S-1360: In vitro activity of a new HIV-1 integrase inhibitor in clinical development
-
Seattle, WA; February 24-28; Abstract 8
-
Yoshinaga, T.; Sato, A.; Fujishita, T.; Fujiwara, T. S-1360: in vitro activity of a new HIV-1 integrase inhibitor in clinical development. Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA; February 24-28, 2002; Abstract 8, p 55.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 55
-
-
Yoshinaga, T.1
Sato, A.2
Fujishita, T.3
Fujiwara, T.4
-
113
-
-
0037076324
-
Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes
-
Grobler, J. A.; Stillmock, K.; Hu, B.; Witmer, M.; Felock, P.; Espeseth, A. S.; Wolfe, A.; Egbertson, M.; Bourgeois, M.; Melamed, J.; Wai, J. S.; Young, S.; Vacca, J.; Hazuda, D. J. Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 6661-6666.
-
(2002)
Proc. Natl. Acad. Sci. U.S.A.
, vol.99
, pp. 6661-6666
-
-
Grobler, J.A.1
Stillmock, K.2
Hu, B.3
Witmer, M.4
Felock, P.5
Espeseth, A.S.6
Wolfe, A.7
Egbertson, M.8
Bourgeois, M.9
Melamed, J.10
Wai, J.S.11
Young, S.12
Vacca, J.13
Hazuda, D.J.14
-
114
-
-
0041353616
-
Metal-dependent inhibition of HIV-1 integrase by β-diketo acids and resistance of the soluble double-mutant (F185K/C280S)
-
Marchand, C.; Johnson, A. A.; Karki, R. G.; Pais, G. C. G.; Zhang, X.; Cowansage, K.; Patel, T. A.; Nicklaus, M. C.; Burke, T. R., Jr.; Pommier, Y. Metal-dependent inhibition of HIV-1 integrase by β-diketo acids and resistance of the soluble double-mutant (F185K/C280S). Mol. Pharmacol. 2003, 64, 600-609.
-
(2003)
Mol. Pharmacol.
, vol.64
, pp. 600-609
-
-
Marchand, C.1
Johnson, A.A.2
Karki, R.G.3
Pais, G.C.G.4
Zhang, X.5
Cowansage, K.6
Patel, T.A.7
Nicklaus, M.C.8
Burke Jr., T.R.9
Pommier, Y.10
-
115
-
-
0034727864
-
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells
-
Wai, J. S.; Egbertson, M. S.; Payne, L. S.; Fisher, T. E.; Embrey, M. W.; Tran, L. O.; Melamed, J. Y.; Langford, H. M.; Guare, J. P., Jr.; Zhuang, L.; Grey, V. E.; Vacca, J. P.; Holloway, M. K.; Naylor-Olsen, A. M.; Hazuda, D. J.; Felock, P. J.; Wolfe, A. L.; Stillmock, K. A.; Schleif, W. A.; Gabryelski, L. J.; Young, S. D. 4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells. J. Med. Chem. 2000, 43, 4923-4926.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 4923-4926
-
-
Wai, J.S.1
Egbertson, M.S.2
Payne, L.S.3
Fisher, T.E.4
Embrey, M.W.5
Tran, L.O.6
Melamed, J.Y.7
Langford, H.M.8
Guare Jr., J.P.9
Zhuang, L.10
Grey, V.E.11
Vacca, J.P.12
Holloway, M.K.13
Naylor-Olsen, A.M.14
Hazuda, D.J.15
Felock, P.J.16
Wolfe, A.L.17
Stillmock, K.A.18
Schleif, W.A.19
Gabryelski, L.J.20
Young, S.D.21
more..
-
116
-
-
0037463757
-
Azido-containing aryl β-diketo acid HIV-1 integrase inhibitors
-
Zhang, X.; Pais, G. C. G.; Svarvskaia, E. S.; Marchand, C.; Johnson, A. A.; Karki, R. G.; Nicklaus, M. C.; Pathak, V. K.; Pommier, Y.; Burke, T. R., Jr. Azido-containing aryl β-diketo acid HIV-1 integrase inhibitors. Bioorg. Med. Chem. Lett. 2003, 13, 1215-1219.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 1215-1219
-
-
Zhang, X.1
Pais, G.C.G.2
Svarvskaia, E.S.3
Marchand, C.4
Johnson, A.A.5
Karki, R.G.6
Nicklaus, M.C.7
Pathak, V.K.8
Pommier, Y.9
Burke Jr., T.R.10
-
117
-
-
0037474193
-
Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid
-
Shaw-Reid, C. A.; Munshi, V.; Graham, P.; Wolfe, A.; Witmer, M.; Danzeisen, R.; Olsen, D. B.; Carroll, S. S.; Embrey, M.; Wai, J. S.; Miller, M. D.; Cole, J. L.; Hazuda, D. J. Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid. J. Biol. Chem. 2003, 278, 2777-2780.
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 2777-2780
-
-
Shaw-Reid, C.A.1
Munshi, V.2
Graham, P.3
Wolfe, A.4
Witmer, M.5
Danzeisen, R.6
Olsen, D.B.7
Carroll, S.S.8
Embrey, M.9
Wai, J.S.10
Miller, M.D.11
Cole, J.L.12
Hazuda, D.J.13
-
118
-
-
0037434509
-
Design and synthesis of 8-hydroxy[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells
-
Zhuang, L.; Wai, J. S.; Embrey, M. W.; Fisher, T. E.; Egbertson, M. S.; Payne, L. S.; Guare, J. P., Jr.; Vacca, J. P.; Hazuda, D. J.; Felock, P. J.; Wolfe, A. L.; Stillmock, K. A.; Witmer, M. V.; Moyer, G.; Schleif, W. A.; Gabryelski, L. J.; Leonard, Y. M.; Lynch, J. J., Jr.; Michelson, S. R.; Young, S. D. Design and synthesis of 8-hydroxy[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. J. Med. Chem. 2003, 46, 453-456.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 453-456
-
-
Zhuang, L.1
Wai, J.S.2
Embrey, M.W.3
Fisher, T.E.4
Egbertson, M.S.5
Payne, L.S.6
Guare Jr., J.P.7
Vacca, J.P.8
Hazuda, D.J.9
Felock, P.J.10
Wolfe, A.L.11
Stillmock, K.A.12
Witmer, M.V.13
Moyer, G.14
Schleif, W.A.15
Gabryelski, L.J.16
Leonard, Y.M.17
Lynch Jr., J.J.18
Michelson, S.R.19
Young, S.D.20
more..
-
119
-
-
0037162281
-
New class of HIV integrase inhibitors that block viral replication in cell culture
-
Pannecouque, C.; Pluymers, W.; Van Maele, B.; Tetz, V.; Cherepanov, P.; De Clercq, E.; Witvrouw, M.; Debyser, Z. New class of HIV integrase inhibitors that block viral replication in cell culture. Curr. Biol. 2002, 12, 1169-1177.
-
(2002)
Curr. Biol.
, vol.12
, pp. 1169-1177
-
-
Pannecouque, C.1
Pluymers, W.2
Van Maele, B.3
Tetz, V.4
Cherepanov, P.5
De Clercq, E.6
Witvrouw, M.7
Debyser, Z.8
-
120
-
-
0033028772
-
Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy
-
Daelemans, D.; Vandamme, A. M.; De Clercq, E. Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy. Antiviral Chem. Chemother. 1999, 10, 1-14.
-
(1999)
Antiviral Chem. Chemother.
, vol.10
, pp. 1-14
-
-
Daelemans, D.1
Vandamme, A.M.2
De Clercq, E.3
-
121
-
-
0034608946
-
Inhibition of the RNA-dependent transactivation and replication of human immunodeficiency virus type 1 by a fluoroquinoline derivative K-37
-
Okamoto, H.; Cujec, T. P.; Okamoto, M.; Peterlin, B. M.; Baba, M.; Okamoto, T. Inhibition of the RNA-dependent transactivation and replication of human immunodeficiency virus type 1 by a fluoroquinoline derivative K-37. Virology 2000, 272, 402-408.
-
(2000)
Virology
, vol.272
, pp. 402-408
-
-
Okamoto, H.1
Cujec, T.P.2
Okamoto, M.3
Peterlin, B.M.4
Baba, M.5
Okamoto, T.6
-
122
-
-
0031893416
-
Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription
-
Turpin, J. A.; Buckheit, R. W., Jr.; Derse, D.; Hollingshead, M.; Williamson, K.; Palamone, C.; Osterling, M. C.; Hill, S. A.; Graham, L.; Schaefer, C. A.; Bu, M.; Huang, M.; Cholody, W. M.; Michejda, C. J.; Rice, W. G. Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription. Antimicrob. Agents Chemother. 1998, 42, 487-494.
-
(1998)
Antimicrob. Agents Chemother.
, vol.42
, pp. 487-494
-
-
Turpin, J.A.1
Buckheit Jr., R.W.2
Derse, D.3
Hollingshead, M.4
Williamson, K.5
Palamone, C.6
Osterling, M.C.7
Hill, S.A.8
Graham, L.9
Schaefer, C.A.10
Bu, M.11
Huang, M.12
Cholody, W.M.13
Michejda, C.J.14
Rice, W.G.15
-
123
-
-
0034665961
-
Flavopiridol inhibits P-TEFb and blocks HIV-1 replication
-
Chao, S. H.; Fujinaga, K.; Marion, J. E.; Taube, R.; Sausville, E. A.; Senderowicz, A. M.; Peterlin, B. M.; Prince, D. H. Flavopiridol inhibits P-TEFb and blocks HIV-1 replication. J. Biol. Chem. 2000, 275, 28345-28348.
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 28345-28348
-
-
Chao, S.H.1
Fujinaga, K.2
Marion, J.E.3
Taube, R.4
Sausville, E.A.5
Senderowicz, A.M.6
Peterlin, B.M.7
Prince, D.H.8
-
124
-
-
0032870371
-
Inhibition of human immunodeficiency virus type 1 replication in acutely and chronically infected cells by EM2487, a novel substance produced by a Streptomyces species
-
Baba, M.; Okamoto, M.; Takeuchi, H. Inhibition of human immunodeficiency virus type 1 replication in acutely and chronically infected cells by EM2487, a novel substance produced by a Streptomyces species. Antimicrob. Agents Chemother. 1999, 43, 2350-2355.
-
(1999)
Antimicrob. Agents Chemother.
, vol.43
, pp. 2350-2355
-
-
Baba, M.1
Okamoto, M.2
Takeuchi, H.3
-
125
-
-
0030976612
-
An inhibitor of the Tat/TAR RNA interaction that effectively suppresses HIV-1 replication
-
Hamy, F.; Felder, E. R.; Heizmann, G.; Lazdins, J.; Aboul-ela, F.; Varani, G.; Karn, J.; Klimkait, T. An inhibitor of the Tat/TAR RNA interaction that effectively suppresses HIV-1 replication. Proc. Natl. Acad. Sci. U.S.A. 1997, 94, 3548-3553.
-
(1997)
Proc. Natl. Acad. Sci. U.S.A.
, vol.94
, pp. 3548-3553
-
-
Hamy, F.1
Felder, E.R.2
Heizmann, G.3
Lazdins, J.4
Aboul-ela, F.5
Varani, G.6
Karn, J.7
Klimkait, T.8
-
126
-
-
0033971512
-
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: Inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry
-
Daelemans, D.; Schols, D.; Witvrouw, M.; Pannecouque, C.; Hatse, S.; van Dooren, S.; Hamy, F.; Klimkait, T.; De Clercq, E.; Vandamme, A.-M. A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry. Mol. Pharmacol. 2000, 57, 116-124.
-
(2000)
Mol. Pharmacol.
, vol.57
, pp. 116-124
-
-
Daelemans, D.1
Schols, D.2
Witvrouw, M.3
Pannecouque, C.4
Hatse, S.5
Van Dooren, S.6
Hamy, F.7
Klimkait, T.8
De Clercq, E.9
Vandamme, A.-M.10
-
127
-
-
0037416975
-
New anti-human immunodeficiency virus type 1 6-aminoquinolones: Mechanism of action
-
Parolin, C.; Gatto, B.; Del Vecchio, C.; Pecere, T.; Tramontano, E.; Cecchetti, V.; Fravolini, A.; Masiero, S.; Palumbo, M.; Palu, G. New anti-human immunodeficiency virus type 1 6-aminoquinolones: mechanism of action. Antimicrob. Agents Chemother. 2003, 47, 889-896.
-
(2003)
Antimicrob. Agents Chemother.
, vol.47
, pp. 889-896
-
-
Parolin, C.1
Gatto, B.2
Del Vecchio, C.3
Pecere, T.4
Tramontano, E.5
Cecchetti, V.6
Fravolini, A.7
Masiero, S.8
Palumbo, M.9
Palu, G.10
-
128
-
-
0036753540
-
Tat stimulates cotranscriptional capping of HIV Mrna
-
Chiu, Y. L.; Ho, C. K.; Saha, N.; Schwer, B.; Shuman, S.; Rana, T. M. Tat stimulates cotranscriptional capping of HIV Mrna. Mol. Cell 2002, 10, 585-597.
-
(2002)
Mol. Cell
, vol.10
, pp. 585-597
-
-
Chiu, Y.L.1
Ho, C.K.2
Saha, N.3
Schwer, B.4
Shuman, S.5
Rana, T.M.6
-
129
-
-
0031439586
-
S-Adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation
-
Daelemans, D.; Esté, J. A.; Witvrouw, M.; Pannecouque, C.; Jonckheere, H.; Aquaro, S.; Perno, C. F.; De Clercq, E.; Vandamme, A.-M. S-Adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation. Mol. Pharmacol. 1997, 52, 1157-1163.
-
(1997)
Mol. Pharmacol.
, vol.52
, pp. 1157-1163
-
-
Daelemans, D.1
Esté, J.A.2
Witvrouw, M.3
Pannecouque, C.4
Jonckheere, H.5
Aquaro, S.6
Perno, C.F.7
De Clercq, E.8
Vandamme, A.-M.9
-
130
-
-
0037195181
-
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export
-
Daelemans, D.; Afonia, E.; Nilsson, J.; Werner, G.; Kjems, J.; De Clercq, E.; Pavlakis, G. N.; Vandamme, A.-M. A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 14440-14445.
-
(2002)
Proc. Natl. Acad. Sci. U.S.A.
, vol.99
, pp. 14440-14445
-
-
Daelemans, D.1
Afonia, E.2
Nilsson, J.3
Werner, G.4
Kjems, J.5
De Clercq, E.6
Pavlakis, G.N.7
Vandamme, A.-M.8
-
131
-
-
0036338304
-
1,2,4-Triazole derivatives inhibiting the human immunodeficiency virus type 1 (HIV-1) in vitro
-
Lagoja, I. M.; Pannecouque, C.; Musumeci, L.; Froeyen, M.; Van Aerschot, A.; Balzarini, J.; Herdewijn, P.; De Clercq, E. 1,2,4-Triazole derivatives inhibiting the human immunodeficiency virus type 1 (HIV-1) in vitro. Helv. Chim. Acta 2002, 85, 1883-1892.
-
(2002)
Helv. Chim. Acta
, vol.85
, pp. 1883-1892
-
-
Lagoja, I.M.1
Pannecouque, C.2
Musumeci, L.3
Froeyen, M.4
Van Aerschot, A.5
Balzarini, J.6
Herdewijn, P.7
De Clercq, E.8
-
132
-
-
0242500883
-
N-Aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action
-
Lagoja, I. M.; Pannecouque, C.; Van Aerschot, A.; Witvrouw, M.; Debyser, Z.; Balzarini, J.; Herdewijn, P.; De Clercq, E. N-Aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action. J. Med. Chem. 2003, 46, 1546-1553.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1546-1553
-
-
Lagoja, I.M.1
Pannecouque, C.2
Van Aerschot, A.3
Witvrouw, M.4
Debyser, Z.5
Balzarini, J.6
Herdewijn, P.7
De Clercq, E.8
-
133
-
-
0041421236
-
Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives
-
Stevens, M.; Pannecouque, C.; De Clercq, E.; Balzarini, J. Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives. Antimicrob. Agents Chemother. 2003, 47, 2951-2957.
-
(2003)
Antimicrob. Agents Chemother.
, vol.47
, pp. 2951-2957
-
-
Stevens, M.1
Pannecouque, C.2
De Clercq, E.3
Balzarini, J.4
-
134
-
-
0141925605
-
Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action
-
Stevens, M.; Pannecouque, C.; De Clercq, E.; Balzarini, J. Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action. Antimicrob. Agents Chemother. 2003, 47, 3109-3116.
-
(2003)
Antimicrob. Agents Chemother.
, vol.47
, pp. 3109-3116
-
-
Stevens, M.1
Pannecouque, C.2
De Clercq, E.3
Balzarini, J.4
-
135
-
-
0033844808
-
In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632
-
Gong, Y. F.; Robinson, B. S.; Rose, R. E.; Deminie, C.; Spicer, T. P.; Stock, D., Colonno, R. J.; Lin, P. F. In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632. Antimicrob. Agents Chemother. 2000, 44, 2319-2326.
-
(2000)
Antimicrob. Agents Chemother.
, vol.44
, pp. 2319-2326
-
-
Gong, Y.F.1
Robinson, B.S.2
Rose, R.E.3
Deminie, C.4
Spicer, T.P.5
Stock, D.6
Colonno, R.J.7
Lin, P.F.8
-
136
-
-
0037379517
-
Activities of atazanavir (BMS-232632) against a large panel of human immunodeficiency virus type 1 clinical isolates resistant to one or more approved protease inhibitors
-
Colonno, R. J.; Thiry, A.; Limoli, K.; Parkin, N. Activities of atazanavir (BMS-232632) against a large panel of human immunodeficiency virus type 1 clinical isolates resistant to one or more approved protease inhibitors. Antimicrob. Agents Chemother. 2003, 47, 1324-1333.
-
(2003)
Antimicrob. Agents Chemother.
, vol.47
, pp. 1324-1333
-
-
Colonno, R.J.1
Thiry, A.2
Limoli, K.3
Parkin, N.4
-
137
-
-
0037661234
-
Therapy with atazanavir plus saquinavir in patients failing highly active antretroviral therapy, a randomized comparative pilot trial
-
Haas, D. W.; Zala, C.; Schrader, S.; Piliero, P.; Jaeger, H.; Nunes, D.; Thiry, A.; Schnittman, S.; Sension, M. Therapy with atazanavir plus saquinavir in patients failing highly active antretroviral therapy, a randomized comparative pilot trial. AIDS 2003, 17, 1339-1349.
-
(2003)
AIDS
, vol.17
, pp. 1339-1349
-
-
Haas, D.W.1
Zala, C.2
Schrader, S.3
Piliero, P.4
Jaeger, H.5
Nunes, D.6
Thiry, A.7
Schnittman, S.8
Sension, M.9
-
138
-
-
0037234238
-
Results of a phase 2 clinical trial at 48 weeks (AI424-007): A dose-ranging, safety, and efficacy comparative trial of atazanavir at three doses in combination with didanosine and stavudine in antiretroviral-naive subjects
-
Sanne, I.; Piliero, P.; Squires, K.; Thiry, A.; Schnittmann, S. Results of a phase 2 clinical trial at 48 weeks (AI424-007): a dose-ranging, safety, and efficacy comparative trial of atazanavir at three doses in combination with didanosine and stavudine in antiretroviral-naive subjects. J. Acquired Immune Defic. Syndr. 2003, 32, 18-29.
-
(2003)
J. Acquired Immune Defic. Syndr.
, vol.32
, pp. 18-29
-
-
Sanne, I.1
Piliero, P.2
Squires, K.3
Thiry, A.4
Schnittmann, S.5
-
139
-
-
14944368002
-
Atazanavir and efavirenz, each combined with fixed-dose zidovudine and lamivudine, have similar effects on body fat distribution in antiretroviral-naïve patients: 48-Week results from the metabolic substudy of BMS AI424-034
-
Paris, France, July 14-17
-
Jemsek, J. G.; Arathoon, E.; Arlotti, M.; Perez, C.; Sosa, N.; Giordano, M.; Thiry, A.; Soccodato, M. Atazanavir and efavirenz, each combined with fixed-dose zidovudine and lamivudine, have similar effects on body fat distribution in antiretroviral-naïve patients: 48-week results from the metabolic substudy of BMS AI424-034. Presented at the 2nd IAS Conference on HIV and Pathogenesis, Paris, France, July 14-17, 2003.
-
(2003)
2nd IAS Conference on HIV and Pathogenesis
-
-
Jemsek, J.G.1
Arathoon, E.2
Arlotti, M.3
Perez, C.4
Sosa, N.5
Giordano, M.6
Thiry, A.7
Soccodato, M.8
-
140
-
-
0036145503
-
A potent human immunodeficiency virus type 1 protease inhibitor, UIC-94003 (TMC-126), and selection of a novel (A28S) mutation in the protease active site
-
Yoshimura, K; Kato, R.; Kavlick, M. F.; Nguyen, A.; Maroun, V.; Maeda, K.; Hussain, K. A.; Ghosh, A. K; Gulnik, S. V.; Erickson, J. W.; Mitsuya, H. A potent human immunodeficiency virus type 1 protease inhibitor, UIC-94003 (TMC-126), and selection of a novel (A28S) mutation in the protease active site. J. Virol. 2002, 76, 1349-1358.
-
(2002)
J. Virol.
, vol.76
, pp. 1349-1358
-
-
Yoshimura, K.1
Kato, R.2
Kavlick, M.F.3
Nguyen, A.4
Maroun, V.5
Maeda, K.6
Hussain, K.A.7
Ghosh, A.K.8
Gulnik, S.V.9
Erickson, J.W.10
Mitsuya, H.11
-
141
-
-
0013409604
-
TMC 114, a highly potent protease inhibitor (PI) with an excellent profile against HIV variants highly resistant to current PIs
-
Chicago, IL, December 16-19 ; Abstract F-1677
-
de Béthune, M.; Wigerinck, P.; Jonckheere, H.; Tahri, A.; Maes, L.; Pauwels, R.; Erickson, J. TMC 114, a highly potent protease inhibitor (PI) with an excellent profile against HIV variants highly resistant to current PIs. Presented at the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Chicago, IL, December 16-19, 2001; Abstract F-1677.
-
(2001)
41st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)
-
-
De Béthune, M.1
Wigerinck, P.2
Jonckheere, H.3
Tahri, A.4
Maes, L.5
Pauwels, R.6
Erickson, J.7
-
142
-
-
0013415974
-
Safety, tolerability and pharmacokinetics of escalating singe oral doses of TMC 114, a novel protease inhibitor (PI) highly active against HIV-1 variants resistant to other PIs
-
Chicago, IL, December 16-19; Abstract I-1934
-
Van Der Geest, R.; Van Der Sandt, I.; Gille, D.; Groen, K.; Tritsmans, L.; Stoffels, P. Safety, tolerability and pharmacokinetics of escalating singe oral doses of TMC 114, a novel protease inhibitor (PI) highly active against HIV-1 variants resistant to other PIs. Presented at the 41st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Chicago, IL, December 16-19, 2001; Abstract I-1934.
-
(2001)
41st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)
-
-
Van Der Geest, R.1
Van Der Sandt, I.2
Gille, D.3
Groen, K.4
Tritsmans, L.5
Stoffels, P.6
-
143
-
-
14944354003
-
TMC114: A new PI
-
Toulon, France, June 3-5; Abstract OP 4.4
-
Lefebvre, E. TMC114: a new PI. Presented at the 13th International Symposium on HIV & Emerging Infectious Diseases, Toulon, France, June 3-5, 2004; Abstract OP 4.4, p 56.
-
(2004)
13th International Symposium on HIV & Emerging Infectious Diseases
, pp. 56
-
-
Lefebvre, E.1
-
144
-
-
0030895692
-
Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor
-
Poppe, S. M.; Slade, D. E.; Chong, K. T.; Hinshaw, R. R.; Pagano, P. J.; Markowitz, M.; Ho, D. D.; Mo, H.; Gorman, R. R., 3rd; Dueweke, T. J.; Thaisrivongs, S.; Tarpley, W. G. Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor. Antimicrob. Agents Chemother. 1997, 41, 1058-1063.
-
(1997)
Antimicrob. Agents Chemother.
, vol.41
, pp. 1058-1063
-
-
Poppe, S.M.1
Slade, D.E.2
Chong, K.T.3
Hinshaw, R.R.4
Pagano, P.J.5
Markowitz, M.6
Ho, D.D.7
Mo, H.8
Gorman III, R.R.9
Dueweke, T.J.10
Thaisrivongs, S.11
Tarpley, W.G.12
-
145
-
-
12944322516
-
Tipranavir (PNU-140690): A potent, orally bioavaible nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class
-
Turner, S. R.; Strohbach, J. W.; Tommasi, R. A.; Aristoff, P. A.; Johnson, P. D.; Skulnick, H. I.; Dolak, L. A.; Seest, E. P.; Tomich, P. K.; Bohanon, M. J.; Horng, M. M.; Lynn, J. C.; Chong, K. T.; Hinshaw, R. R.; Watenpaugh, K. D.; Janakiraman, M. N.; Thaisrivongs, S. Tipranavir (PNU-140690): a potent, orally bioavaible nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. J. Med. Chem. 1998, 41, 3467-3476.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 3467-3476
-
-
Turner, S.R.1
Strohbach, J.W.2
Tommasi, R.A.3
Aristoff, P.A.4
Johnson, P.D.5
Skulnick, H.I.6
Dolak, L.A.7
Seest, E.P.8
Tomich, P.K.9
Bohanon, M.J.10
Horng, M.M.11
Lynn, J.C.12
Chong, K.T.13
Hinshaw, R.R.14
Watenpaugh, K.D.15
Janakiraman, M.N.16
Thaisrivongs, S.17
-
146
-
-
0034623020
-
Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples
-
Larder, B. A.; Hertogs, K.; Bloor, S.; van den Eynde, C. H.; DeCian, W.; Wang, Y.; Freimuth, W. W.; Tarpley, G. Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples. AIDS 2000, 14, 1943-1948.
-
(2000)
AIDS
, vol.14
, pp. 1943-1948
-
-
Larder, B.A.1
Hertogs, K.2
Bloor, S.3
Van Den Eynde, C.H.4
Decian, W.5
Wang, Y.6
Freimuth, W.W.7
Tarpley, G.8
-
147
-
-
0034053044
-
Susceptibility to PNU-140690 (tipranavir) of human immunodeficiency virus type 1 isolates derived from patients with multidrug resistance to other protease inhibitors
-
Rusconi, S.; La Seta Catamancio, S.; Citterio, P.; Kurtagic, S.; Violin, M.; Balotta, C.; Moroni, M.; Galli, M.; d'Arminio-Monforte, A. Susceptibility to PNU-140690 (tipranavir) of human immunodeficiency virus type 1 isolates derived from patients with multidrug resistance to other protease inhibitors. Antimicrob. Agents Chemother. 2000, 44, 1328-1332.
-
(2000)
Antimicrob. Agents Chemother.
, vol.44
, pp. 1328-1332
-
-
Rusconi, S.1
La Seta Catamancio, S.2
Citterio, P.3
Kurtagic, S.4
Violin, M.5
Balotta, C.6
Moroni, M.7
Galli, M.8
D'Arminio-Monforte, A.9
-
148
-
-
0038746300
-
An open-label steady state investigation of the pharmacokinetics (PK) of tipranavir (TPV) and ritonavir (RTV) and their effects on cytochrome P-450 (3A4) activity in normal health volunteers (BI 1182.5)
-
Seattle, WA, February 24-28; Abstract 434-W
-
McCallister, S.; Sabo, J.; Galitz, L.; Mayers, D. An open-label steady state investigation of the pharmacokinetics (PK) of tipranavir (TPV) and ritonavir (RTV) and their effects on cytochrome P-450 (3A4) activity in normal health volunteers (BI 1182.5). Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002; Abstract 434-W.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
-
-
McCallister, S.1
Sabo, J.2
Galitz, L.3
Mayers, D.4
-
149
-
-
0038746305
-
Resistance to tipranavir is uncommon in a randomized trial of tipranavir/ritonavir (TPV/RTV) in multiple PI-failure patients (BI 1182.2)
-
Seattle, WA, February 24-28; Abstract 562-T
-
Schwartz, R.; Kazanjian, P.; Slater, L.; Hathaway, B.; Markowitz, M.; Wheeler, D.; Goldman, M.; Drulak, M.; McCallister, S.; Mayers, D. Resistance to tipranavir is uncommon in a randomized trial of tipranavir/ritonavir (TPV/RTV) in multiple PI-failure patients (BI 1182.2). Presented at the 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002; Abstract 562-T, p 261.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
, pp. 261
-
-
Schwartz, R.1
Kazanjian, P.2
Slater, L.3
Hathaway, B.4
Markowitz, M.5
Wheeler, D.6
Goldman, M.7
Drulak, M.8
McCallister, S.9
Mayers, D.10
-
150
-
-
0036221012
-
Inhibitory effects of quinones on RNase H activity associated HIV-1 reverse transcriptase
-
Min, B. S.; Miyashiro, H.; Hattori, M. Inhibitory effects of quinones on RNase H activity associated HIV-1 reverse transcriptase. Phytother. Res. 2002, 16 (Suppl. 1), S57-S62.
-
(2002)
Phytother. Res.
, vol.16
, Issue.SUPPL. 1
-
-
Min, B.S.1
Miyashiro, H.2
Hattori, M.3
-
151
-
-
0036049662
-
HIV-1 integrase and RNase H activities as therapeutic targets
-
Andreola, M. L.; Soultrait, V. R.; Desjobert, C.; Parissi, V.; Andreola, M.; Fournier, M.; Litvak, S. HIV-1 integrase and RNase H activities as therapeutic targets. Expert Opin. Ther. Targets 2002, 6, 433-446.
-
(2002)
Expert Opin. Ther. Targets
, vol.6
, pp. 433-446
-
-
Andreola, M.L.1
Soultrait, V.R.2
Desjobert, C.3
Parissi, V.4
Andreola, M.5
Fournier, M.6
Litvak, S.7
-
152
-
-
0036822181
-
Uncovering the complexities of retroviral ribonuclease H reveals its potential as a therapeutic target
-
Klarmann, G. J.; Hawkins, M. E.; Le Grice, S. F. Uncovering the complexities of retroviral ribonuclease H reveals its potential as a therapeutic target. AIDS Rev. 2002, 4, 183-194.
-
(2002)
AIDS Rev.
, vol.4
, pp. 183-194
-
-
Klarmann, G.J.1
Hawkins, M.E.2
Le Grice, S.F.3
-
153
-
-
0037474193
-
Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-benzoylaminothien-2-yl]-2,4-dioxobutanoic acid
-
Shaw-Reid, C. A.; Munshi, V.; Graham, P.; Wolfe, A.; Witmer, M.; Danzeisen, R.; Olsen, D. B.; Carroll, S. S.; Embrey, M.; Wai, J. S.; Miller, M. D.; Cole, J. L.; Hazuda, D. J. Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid. J. Biol. Chem. 2003, 278, 2777-2780.
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 2777-2780
-
-
Shaw-Reid, C.A.1
Munshi, V.2
Graham, P.3
Wolfe, A.4
Witmer, M.5
Danzeisen, R.6
Olsen, D.B.7
Carroll, S.S.8
Embrey, M.9
Wai, J.S.10
Miller, M.D.11
Cole, J.L.12
Hazuda, D.J.13
-
154
-
-
10744226166
-
Two-metal-ion mechanism of RNA cleavage by HIV RNase H and mechanism based design of selective HIV RNase H inhibitors
-
Klumpp, K.; Hang, J. Q.; Rajendran, S.; Yang, Y.; Derosier, A.; Wong Kai In, P.; Overton, H.; Parkes, K. E. B.; Cammack, N.; Martin, J. A. Two-metal-ion mechanism of RNA cleavage by HIV RNase H and mechanism based design of selective HIV RNase H inhibitors. Nucleic Acids Res. 2003, 31, 6852-6859.
-
(2003)
Nucleic Acids Res.
, vol.31
, pp. 6852-6859
-
-
Klumpp, K.1
Hang, J.Q.2
Rajendran, S.3
Yang, Y.4
Derosier, A.5
Wong Kai In, P.6
Overton, H.7
Parkes, K.E.B.8
Cammack, N.9
Martin, J.A.10
-
155
-
-
11144355815
-
Activity of the isolated HIV RNase H domain and specific inhibition by N-hydroxyimides
-
Hang, J. Q.; Rajendran, S.; Yang, Y.; Li, Y.; Wong Kai In, P.; Overton, H.; Parkes, K. E. B.; Cammack, N.; Martin, J. A.; Klumpp, K. Activity of the isolated HIV RNase H domain and specific inhibition by N-hydroxyimides. Biochem. Biophys. Res. Commun. 2004, 317, 321-329.
-
(2004)
Biochem. Biophys. Res. Commun.
, vol.317
, pp. 321-329
-
-
Hang, J.Q.1
Rajendran, S.2
Yang, Y.3
Li, Y.4
Wong Kai In, P.5
Overton, H.6
Parkes, K.E.B.7
Cammack, N.8
Martin, J.A.9
Klumpp, K.10
-
156
-
-
0037542551
-
Once-a-day highly active antiretroviral therapy: A systemic review
-
Ena, J.; Pasquau, F. Once-a-day highly active antiretroviral therapy: a systemic review. Clin. Infect. Dis. 2003, 36, 1186-1190.
-
(2003)
Clin. Infect. Dis.
, vol.36
, pp. 1186-1190
-
-
Ena, J.1
Pasquau, F.2
-
157
-
-
0037444053
-
Determining the relative efficacy of highly active antiretroviral therapy
-
Louie, M.; Hogan, C.; Di Mascio, M.; Hurley, A.; Simon, V.; Rooney, J.; Ruiz, N.; Brun, S.; Sun, E.; Perelson, A. S.; Ho, D. D.; Markowitz, M. Determining the relative efficacy of highly active antiretroviral therapy. J. Infect. Dis. 2003, 187, 896-900.
-
(2003)
J. Infect. Dis.
, vol.187
, pp. 896-900
-
-
Louie, M.1
Hogan, C.2
Di Mascio, M.3
Hurley, A.4
Simon, V.5
Rooney, J.6
Ruiz, N.7
Brun, S.8
Sun, E.9
Perelson, A.S.10
Ho, D.D.11
Markowitz, M.12
-
158
-
-
2342537759
-
Triple-nucleoside regimens versus efavirenz-containing regimens for the initial treatment of HIV-1 infection
-
Gulick, R. M.; Heather, M. P. H.; Ribaudo, H. J.; Shikuma, C. M.; Lustgarten, S.; Squires, K. E.; Meyer, W. A., III; Acosta, E. P.; Schackman, B. R.; Pilcher, C. D.; Murphy, R. L.; Maher, W. E.; Witt, M. D.; Reichman, R. C.; Snyder, S.; Klingman, K. L.; Kuritzkes, D. R. Triple-nucleoside regimens versus efavirenz-containing regimens for the initial treatment of HIV-1 infection. N. Engl. J. Med. 2004, 350, 1850-1861.
-
(2004)
N. Engl. J. Med.
, vol.350
, pp. 1850-1861
-
-
Gulick, R.M.1
Heather, M.P.H.2
Ribaudo, H.J.3
Shikuma, C.M.4
Lustgarten, S.5
Squires, K.E.6
Meyer III, W.A.7
Acosta, E.P.8
Schackman, B.R.9
Pilcher, C.D.10
Murphy, R.L.11
Maher, W.E.12
Witt, M.D.13
Reichman, R.C.14
Snyder, S.15
Klingman, K.L.16
Kuritzkes, D.R.17
-
159
-
-
0036569234
-
A randomized trial of simplified maintenance therapy with abacavir, lamivudine, and zidovudine in human immunodeficiency virus infection
-
Opravil, M.; Hirschel, B.; Lazzarin, A.; Furrer, H.; Chave, J.-P.; Yerly, S.; Bisset, L. R.; Fischer, M.; Vernazza, P.; Bernasconi, E.; Battegay, M.; Ledergerber, B.; Günthard, H.; Howe, C.; Weber, R.; Perrin, L. A randomized trial of simplified maintenance therapy with abacavir, lamivudine, and zidovudine in human immunodeficiency virus infection. J. Infect. Dis. 2002, 185, 1251-1260.
-
(2002)
J. Infect. Dis.
, vol.185
, pp. 1251-1260
-
-
Opravil, M.1
Hirschel, B.2
Lazzarin, A.3
Furrer, H.4
Chave, J.-P.5
Yerly, S.6
Bisset, L.R.7
Fischer, M.8
Vernazza, P.9
Bernasconi, E.10
Battegay, M.11
Ledergerber, B.12
Günthard, H.13
Howe, C.14
Weber, R.15
Perrin, L.16
-
160
-
-
11144357656
-
Comparison of first-line antiretroviral therapy with regimens including nevirapine, efavirenz, or both drugs, plus stavudine and lamivudine: A randomised open-label trial, the 2NN study
-
van Leth, F.; Phanuphak, P.; Ruxrungtham, K.; Baraldi, E.; Miller, S.; Gazzard, B.; Cahn, P.; Lalloo, U. G.; van der Westhuizen, I. P.; Malan, D. R.; Johnson, M. A.; Santos, B. R.; Mulcahy, F.; Wood, R.; Levi, G. C.; Reboredo, G.; Squires, K.; Cassetti, I.; Petit, D.; Raffi, F.; Katlama, C.; Murphy, R. L.; Dam, J. P.; Hassink, E.; van Leeuwen, R.; Robinson, P.; Wit, F. W.; Lange, J. M. A. Comparison of first-line antiretroviral therapy with regimens including nevirapine, efavirenz, or both drugs, plus stavudine and lamivudine: a randomised open-label trial, the 2NN study. Lancet 2004, 363, 1253-1263.
-
(2004)
Lancet
, vol.363
, pp. 1253-1263
-
-
Leth, F.1
Phanuphak, P.2
Ruxrungtham, K.3
Baraldi, E.4
Miller, S.5
Gazzard, B.6
Cahn, P.7
Lalloo, U.G.8
Van Der Westhuizen, I.P.9
Malan, D.R.10
Johnson, M.A.11
Santos, B.R.12
Mulcahy, F.13
Wood, R.14
Levi, G.C.15
Reboredo, G.16
Squires, K.17
Cassetti, I.18
Petit, D.19
Raffi, F.20
Katlama, C.21
Murphy, R.L.22
Dam, J.P.23
Hassink, E.24
Van Leeuwen, R.25
Robinson, P.26
Wit, F.W.27
Lange, J.M.A.28
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