-
1
-
-
0028952146
-
HIV population dynamics in vivo: Implications for genetic variation, pathogenesis, and therapy
-
Coffin, J. M. HIV population dynamics in vivo: Implications for genetic variation, pathogenesis, and therapy. Science 1995, 267, 483-489.
-
(1995)
Science
, vol.267
, pp. 483-489
-
-
Coffin, J.M.1
-
2
-
-
15444369799
-
Global summary of the HIV/AIDS epidemic
-
December
-
WHO/UNAIDS. Global summary of the HIV/AIDS epidemic. WHO report (December 2002). http://www.who.int/hiv/pub/epidemiology/epi2002/en/
-
(2002)
WHO Report
-
-
-
4
-
-
0001707601
-
3′-Azido-3′-deoxythymidine (BW A509U): An antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro
-
Mitsuya, H.; Weinhold, K. J.; Furman, P. A.; St Clair, M. H.; Lehrman, S. N.; Gallo, R. C.; Bolognesi, D.; Barry, D. W.; Broder, S. 3′-Azido- 3′-deoxythymidine (BW A509U): An antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proc. Natl. Acad. Sci. U.S.A. 1985, 82, 7096-7100.
-
(1985)
Proc. Natl. Acad. Sci. U.S.A.
, vol.82
, pp. 7096-7100
-
-
Mitsuya, H.1
Weinhold, K.J.2
Furman, P.A.3
St Clair, M.H.4
Lehrman, S.N.5
Gallo, R.C.6
Bolognesi, D.7
Barry, D.W.8
Broder, S.9
-
5
-
-
0023091963
-
Strategies for antiviral therapy in AIDS
-
Mitsuya, H.; Broder, S. Strategies for antiviral therapy in AIDS. Nature 1987, 325, 773-778.
-
(1987)
Nature
, vol.325
, pp. 773-778
-
-
Mitsuya, H.1
Broder, S.2
-
6
-
-
0024310253
-
Multiple mutations in HIV-1 reverse transcriptase confer high-level resistance to zidovudine (AZT)
-
Larder, B. A.; Kemp, S. D. Multiple mutations in HIV-1 reverse transcriptase confer high-level resistance to zidovudine (AZT). Science 1989, 246, 1155-1158.
-
(1989)
Science
, vol.246
, pp. 1155-1158
-
-
Larder, B.A.1
Kemp, S.D.2
-
8
-
-
0002296754
-
Reverse transcriptase and the generation of retroviral DNA
-
Coffin, J. M., Hughes, S. H., Varmus, H. E., Eds.; Cold Spring Harbor Laboratory Press: Cold Spring Harbor, NY
-
Telesnitsky, A.; Goff, S. P. Reverse transcriptase and the generation of retroviral DNA. In Retroviruses; Coffin, J. M., Hughes, S. H., Varmus, H. E., Eds.; Cold Spring Harbor Laboratory Press: Cold Spring Harbor, NY., 1997; pp 121-160.
-
(1997)
Retroviruses
, pp. 121-160
-
-
Telesnitsky, A.1
Goff, S.P.2
-
9
-
-
0031037916
-
The art of 'HAART': Researchers probe the potential and limits of aggressive HIV treatments
-
Stephenson, J. The art of 'HAART': Researchers probe the potential and limits of aggressive HIV treatments. JAMA 1997, 277, 614-616.
-
(1997)
JAMA
, vol.277
, pp. 614-616
-
-
Stephenson, J.1
-
10
-
-
0032585904
-
The picture of future therapy
-
Gazzard, B. The picture of future therapy. Int. J. Clin. Pract. Suppl. 1999, 103, 45-48.
-
(1999)
Int. J. Clin. Pract. Suppl.
, vol.103
, pp. 45-48
-
-
Gazzard, B.1
-
11
-
-
0038576281
-
Enfuvirtide, an HIV-1 Fusion Inhibitor, for Drug-Resistant HIV Infection in North and South America
-
TORO 1 Study Group
-
Lalezari, J. P.; Henry, K.; O'Hearn, M.; Montaner, J. S.; 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. TORO 1 Study Group. 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.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
-
12
-
-
0036846898
-
New anti-HIV agents and targets
-
De Clercq, E. New anti-HIV agents and targets. Med. Res. Rev. 2002, 22, 531-565
-
(2002)
Med. Res. Rev.
, vol.22
, pp. 531-565
-
-
De Clercq, E.1
-
13
-
-
17944374798
-
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues
-
Ludovici, D. W.; De Corte, B. L.; Kukla, M. J.; Ye, H.; Ho C. Y.; Lichtenstein, M. A.; Kavash, R. W.; Andries, K.; de Bethune, M.-P.; Azijn, H.; Pauwels, R.; Lewi, P. J.; Heeres, J.; Koymans, L. M.; de Jonge, M. R.; Van Aken, K. J.; Daeyaert, F. F.; Das, K.; Arnold, E.; Janssen, P. A. Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. Bioorg. Med. Chem. Lett. 2001, 11, 2235-2239.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2235-2239
-
-
Ludovici, D.W.1
De Corte, B.L.2
Kukla, M.J.3
Ye, H.4
Ho, C.Y.5
Lichtenstein, M.A.6
Kavash, R.W.7
Andries, K.8
De Bethune, M.-P.9
Azijn, H.10
Pauwels, R.11
Lewi, P.J.12
Heeres, J.13
Koymans, L.M.14
De Jonge, M.R.15
Van Aken, K.J.16
Daeyaert, F.F.17
Das, K.18
Arnold, E.19
Janssen, P.A.20
more..
-
14
-
-
0025014499
-
Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives
-
Pauwels, R.; Andries, K.; Desmyter, J.; Schols, D.; Kukla, M. J.; Breslin, H. J.; Raeymaeckers, A.; Van Gelder, J.; Woestenborghs, R.; Heykants, J.; Schellekens, K.; Janssen, M. A. C.; De Clercq, E.; Janssen, P. A. J. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature 1990, 343, 470-474.
-
(1990)
Nature
, vol.343
, pp. 470-474
-
-
Pauwels, R.1
Andries, K.2
Desmyter, J.3
Schols, D.4
Kukla, M.J.5
Breslin, H.J.6
Raeymaeckers, A.7
Van Gelder, J.8
Woestenborghs, R.9
Heykants, J.10
Schellekens, K.11
Janssen, M.A.C.12
De Clercq, E.13
Janssen, P.A.J.14
-
15
-
-
0027407551
-
Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase
-
Pauwels, R.; Andries, K.; Debyser, Z.; Daele, P. V.; Schols, D.; Stoffels, P.; Vreese, K. D.; Woestenborghs, R.; Vandamme, A.; Janssen, C. G. M.; Anne, J.; Cauwenbergh, G.; Desmyter, J.; Heykants, J.; Janssen, M. A. C.; De Clercq, E.; Janssen, P. A. J. Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of alpha-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 1711-1715.
-
(1993)
Proc. Natl. Acad. Sci. U.S.A.
, vol.90
, pp. 1711-1715
-
-
Pauwels, R.1
Andries, K.2
Debyser, Z.3
Daele, P.V.4
Schols, D.5
Stoffels, P.6
Vreese, K.D.7
Woestenborghs, R.8
Vandamme, A.9
Janssen, C.G.M.10
Anne, J.11
Cauwenbergh, G.12
Desmyter, J.13
Heykants, J.14
Janssen, M.A.C.15
De Clercq, E.16
Janssen, P.A.J.17
-
16
-
-
17944376896
-
Evolution of anti-HIV drug candidates. Part 1: From alpha- Anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU)
-
Ludovici, D. W.; Kukla, M. J.; Grous, P. G.; Krishnan, S.; Andries, K.; de Béthune, M.-P.; Azijn, H.; Pauwels, R.; De Clercq, E.; Arnold, E.; Janssen, P. A. J. Evolution of anti-HIV drug candidates. Part 1: From alpha- Anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU). Bioorg. Med. Chem. Lett. 2001, 11, 2225-2228.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2225-2228
-
-
Ludovici, D.W.1
Kukla, M.J.2
Grous, P.G.3
Krishnan, S.4
Andries, K.5
De Béthune, M.-P.6
Azijn, H.7
Pauwels, R.8
De Clercq, E.9
Arnold, E.10
Janssen, P.A.J.11
-
17
-
-
17944366732
-
Evolution of anti-HIV drug candidates Part 2: Diaryltriazine (DATA) analogues
-
Ludovici, D. W.; Kavash, R. W.; Kukla, M. J.; Ho, C. Y.; Ye, H.; De Corte, B. L.; Andries, K.; de Béthune, M.-P.; Azijn, H.; Pauwels, R.; Moereels, H. E.; Heeres, J.; Koymans, L. M.; de Jonge, M. R.; Van Aken, K. J.; Daeyaert, F. F.; Lewi, P. J.; Das, K.; Arnold, E.; Janssen, P. A. J. Evolution of anti-HIV drug candidates Part 2: Diaryltriazine (DATA) analogues. Bioorg. Med. Chem. Lett. 2001, 11, 2229-2234.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2229-2234
-
-
Ludovici, D.W.1
Kavash, R.W.2
Kukla, M.J.3
Ho, C.Y.4
Ye, H.5
De Corte, B.L.6
Andries, K.7
De Béthune, M.-P.8
Azijn, H.9
Pauwels, R.10
Moereels, H.E.11
Heeres, J.12
Koymans, L.M.13
De Jonge, M.R.14
Van Aken, K.J.15
Daeyaert, F.F.16
Lewi, P.J.17
Das, K.18
Arnold, E.19
Janssen, P.A.J.20
more..
-
18
-
-
0004169064
-
TMC120, a New Non- Nucleoside Reverse Transcriptase Inhibitor, Is a Potent Antiretroviral in Treatment Naive, HIV-1 Infected Subjects
-
Chicago, IL, February 4-8, Abstract 13
-
Gruzdev, B.; Horban, A.; Boron-Kaczmarska, A.; Gille, D.; van 't Klooster, G.; Pauwels, R. TMC120, a New Non- Nucleoside Reverse Transcriptase Inhibitor, Is a Potent Antiretroviral in Treatment Naive, HIV-1 Infected Subjects. 8th Conference on Retroviruses and Opportunistic Infections, Chicago, IL, February 4-8, 2001. Abstract 13.
-
(2001)
8th Conference on Retroviruses and Opportunistic Infections
-
-
Gruzdev, B.1
Horban, A.2
Boron-Kaczmarska, A.3
Gille, D.4
Van 't Klooster, G.5
Pauwels, R.6
-
19
-
-
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. 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002. Abstract 5.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
-
-
Sankatsing, S.1
Weverling, G.2
Van 't Klooster, G.3
Prins, J.4
Lange, J.5
-
20
-
-
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.; Staszwski, 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. 9th Conference on Retroviruses and Opportunistic Infections, Seattle, WA, February 24-28, 2002. Abstract 4.
-
(2002)
9th Conference on Retroviruses and Opportunistic Infections
-
-
Gazzard, B.1
Pozniak, A.2
Arasteh, K.3
Staszwski, 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
-
21
-
-
0026693137
-
Crystal structure at 3.5 Å resolution of HIV-1 reverse transcriptase complexed with an inhibitor
-
Kohlstaedt, L. A.; Wang, J.; Friedman, J. M.; Rice, P. A.; Steitz, T. A. Crystal structure at 3.5 Å resolution of HIV-1 reverse transcriptase complexed with an inhibitor. Science 1992, 256, 1783-1790.
-
(1992)
Science
, vol.256
, pp. 1783-1790
-
-
Kohlstaedt, L.A.1
Wang, J.2
Friedman, J.M.3
Rice, P.A.4
Steitz, T.A.5
-
22
-
-
0027318776
-
Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A resolution shows bent DNA
-
Jacobo-Molina, A.; Ding, J.; Nanni, R. G.; Clark, A. D., Jr.; Lu, X.; Tantillo, C.; Williams, R. L.; Kamer, G.; Ferris, A. L.; Clark, P.; Hizi, A.; Hughes, S. H.; Arnold, E. Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A resolution shows bent DNA. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6320-6324.
-
(1993)
Proc. Natl. Acad. Sci. U.S.A.
, vol.90
, pp. 6320-6324
-
-
Jacobo-Molina, A.1
Ding, J.2
Nanni, R.G.3
Clark Jr., A.D.4
Lu, X.5
Tantillo, C.6
Williams, R.L.7
Kamer, G.8
Ferris, A.L.9
Clark, P.10
Hizi, A.11
Hughes, S.H.12
Arnold, E.13
-
23
-
-
0029521420
-
The role of nucleic acid in the resistance of HIV-1 reverse transcriptase to nucleoside and nonnucleoside inhibitors
-
Hsiou, Y.; Das, K.; Ding, J.; Tantillo, C.; Boyer, P. L.; Hughes, S. H.; Arnold, E. The role of nucleic acid in the resistance of HIV-1 reverse transcriptase to nucleoside and nonnucleoside inhibitors. Med. Biol. Environ. 1995, 23, 209-215.
-
(1995)
Med. Biol. Environ.
, vol.23
, pp. 209-215
-
-
Hsiou, Y.1
Das, K.2
Ding, J.3
Tantillo, C.4
Boyer, P.L.5
Hughes, S.H.6
Arnold, E.7
-
24
-
-
0028842293
-
The structure of unliganded reverse transcriptase from the human immunodeficiency virus type 1
-
Rodgers, D. W.; Gamblin, S. J.; Harris, B. A.; Ray, S.; Culp, J. S.; Hellmig, B.; Woolf, D. J.; Debouck, C.; Harrison, S. C. The structure of unliganded reverse transcriptase from the human immunodeficiency virus type 1. Proc. Natl. Acad. Sci. U.S.A. 1995, 92, 1222-1226.
-
(1995)
Proc. Natl. Acad. Sci. U.S.A.
, vol.92
, pp. 1222-1226
-
-
Rodgers, D.W.1
Gamblin, S.J.2
Harris, B.A.3
Ray, S.4
Culp, J.S.5
Hellmig, B.6
Woolf, D.J.7
Debouck, C.8
Harrison, S.C.9
-
25
-
-
0029075207
-
Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors
-
Ding, J.; Das, K.; Moereels, H.; Koymans, L.; Andries, K.; Janssen, P. A. J.; Hughes, S. H.; Arnold, E. Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nat. Struct. Biol. 1995, 2, 407-415.
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 407-415
-
-
Ding, J.1
Das, K.2
Moereels, H.3
Koymans, L.4
Andries, K.5
Janssen, P.A.J.6
Hughes, S.H.7
Arnold, E.8
-
26
-
-
0029644484
-
Structure of HIV-1 reverse transcriptase in a complex with the non- nucleoside inhibitor alpha-APA R 95845 at 2.8 Å resolution
-
Ding, J.; Das, K.; Tantillo, C.; Zhang, W.; Clark, A. D., Jr.; Jessen, S.; Lu, X.; Hsiou, Y.; Jacobo-Molina, A.; Andries, K.; Pauwels, R.; Moereels, H.; Koymans, L.; Janssen, P. A. J.; Smith, R. H., Jr.; Kroeger Smith, M. B.; Koepke, M.; Michejda, C. J.; Hughes, S. H.; Arnold, E. Structure of HIV-1 reverse transcriptase in a complex with the non- nucleoside inhibitor alpha-APA R 95845 at 2.8 Å resolution. Structure 1995, 3, 365-379.
-
(1995)
Structure
, vol.3
, pp. 365-379
-
-
Ding, J.1
Das, K.2
Tantillo, C.3
Zhang, W.4
Clark Jr., A.D.5
Jessen, S.6
Lu, X.7
Hsiou, Y.8
Jacobo-Molina, A.9
Andries, K.10
Pauwels, R.11
Moereels, H.12
Koymans, L.13
Janssen, P.A.J.14
Smith Jr., R.H.15
Kroeger Smith, M.B.16
Koepke, M.17
Michejda, C.J.18
Hughes, S.H.19
Arnold, E.20
more..
-
27
-
-
0029645409
-
The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: Lessons for inhibitor design
-
Ren, J.; Esnouf, R.; Hopkins, A.; Ross, C.; Jones, Y.; Stammers, D.; Stuart, D. The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: Lessons for inhibitor design. Structure 1995, 3, 915-926.
-
(1995)
Structure
, vol.3
, pp. 915-926
-
-
Ren, J.1
Esnouf, R.2
Hopkins, A.3
Ross, C.4
Jones, Y.5
Stammers, D.6
Stuart, D.7
-
28
-
-
0030596068
-
Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the Tyr181Cys HIV-1 RT drug-resistant mutant
-
Das, K.; Ding, J.; Hsiou, Y.; Clark, A. D., Jr.; Moereels, H.; Koymans, L.; Andries, K.; Pauwels, R.; Janssen, P. A. J.; Boyer, P. L.; Clark, P.; Smith, R. H., Jr.; Smith, M. B. K.; Michejda, C. J.; Hughes, S. H.; Arnold, E. Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the Tyr181Cys HIV-1 RT drug-resistant mutant. J. Mol. Biol. 1986, 264, 1085-1100.
-
(1986)
J. Mol. Biol.
, vol.264
, pp. 1085-1100
-
-
Das, K.1
Ding, J.2
Hsiou, Y.3
Clark Jr., A.D.4
Moereels, H.5
Koymans, L.6
Andries, K.7
Pauwels, R.8
Janssen, P.A.J.9
Boyer, P.L.10
Clark, P.11
Smith Jr., R.H.12
Smith, M.B.K.13
Michejda, C.J.14
Hughes, S.H.15
Arnold, E.16
-
29
-
-
0029976422
-
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent nonnucleoside inhibitors
-
Hopkins, A. L.; Ren, J.; Esnouf, R. M.; Willcox, B. E.; Jones, E. Y.; Ross, C.; Miyasaka, T.; Walker, R. T.; Tanaka, H.; Stammers, D. K.; Stuart, D. I. Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent nonnucleoside inhibitors. J. Med. Chem. 1996, 39, 1589-1600.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 1589-1600
-
-
Hopkins, A.L.1
Ren, J.2
Esnouf, R.M.3
Willcox, B.E.4
Jones, E.Y.5
Ross, C.6
Miyasaka, T.7
Walker, R.T.8
Tanaka, H.9
Stammers, D.K.10
Stuart, D.I.11
-
30
-
-
13144282707
-
Structures of Tyr188Leu mutant and wild-type HIV-1 reverse transcriptase complexed with the nonnucleoside inhibitor HBY 097: Inhibitor flexibility is a useful design feature for reducing drug resistance
-
Hsiou, Y.; Das, K.; Ding, J.; Clark, A. D., Jr.; Kleim, J. P.; Rosner, M.; Winkler, I.; Riess, G.; Hughes, S. H.; Arnold, E. Structures of Tyr188Leu mutant and wild-type HIV-1 reverse transcriptase complexed with the nonnucleoside inhibitor HBY 097: Inhibitor flexibility is a useful design feature for reducing drug resistance. J. Mol. Biol. 1998, 284, 313-323.
-
(1998)
J. Mol. Biol.
, vol.284
, pp. 313-323
-
-
Hsiou, Y.1
Das, K.2
Ding, J.3
Clark Jr., A.D.4
Kleim, J.P.5
Rosner, M.6
Winkler, I.7
Riess, G.8
Hughes, S.H.9
Arnold, E.10
-
31
-
-
0033598368
-
Crystallographic analysis of the binding modes of thiazoloisoindolinone nonnucleoside inhibitors to HIV-1 reverse transcriptase and comparison with modeling studies
-
Ren, J.; Esnouf, R. M.; Hopkins, A. L.; Stuart, D. I.; Stammers, D. K. Crystallographic analysis of the binding modes of thiazoloisoindolinone nonnucleoside inhibitors to HIV-1 reverse transcriptase and comparison with modeling studies. J. Med. Chem. 1999, 42, 3845-3851.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 3845-3851
-
-
Ren, J.1
Esnouf, R.M.2
Hopkins, A.L.3
Stuart, D.I.4
Stammers, D.K.5
-
32
-
-
0033621167
-
Lamivudine (3TC) resistance in HIV-1 reverse transcriptase involves steric hindrance with beta-branched amino acids
-
Sarafianos, S. G.; Das, K.; Clark, A. D., Jr.; Ding, J.; Boyer, P. L.; Hughes, S. H.; Arnold, E. Lamivudine (3TC) resistance in HIV-1 reverse transcriptase involves steric hindrance with beta-branched amino acids. Proc. Natl. Acad. Sci. U.S.A. 1999, 96, 10027-10032.
-
(1999)
Proc. Natl. Acad. Sci. U.S.A.
, vol.96
, pp. 10027-10032
-
-
Sarafianos, S.G.1
Das, K.2
Clark Jr., A.D.3
Ding, J.4
Boyer, P.L.5
Hughes, S.H.6
Arnold, E.7
-
33
-
-
0034435564
-
Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase
-
Ren, J.; Milton, J.; Weaver, K. L.; Short, S. A.; Stuart, D. I.; Stammers, D. K. Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase. Structure Fold Des. 2000, 8, 1089-1094.
-
(2000)
Structure Fold Des.
, vol.8
, pp. 1089-1094
-
-
Ren, J.1
Milton, J.2
Weaver, K.L.3
Short, S.A.4
Stuart, D.I.5
Stammers, D.K.6
-
34
-
-
0035368238
-
The Lys103Asn mutation of HIV-1 RT: A novel mechanism of drug resistance
-
Hsiou, Y.; Ding, J.; Das, K.; Clark, A. D., Jr.; Boyer, P. L.; Lewi, P.; Janssen, P. A.; Kleim, J. P.; Rosner, M.; Hughes, S. H.; Arnold, E. The Lys103Asn mutation of HIV-1 RT: A novel mechanism of drug resistance. J. Mol. Biol. 2001, 309, 437-445.
-
(2001)
J. Mol. Biol.
, vol.309
, pp. 437-445
-
-
Hsiou, Y.1
Ding, J.2
Das, K.3
Clark Jr., A.D.4
Boyer, P.L.5
Lewi, P.6
Janssen, P.A.7
Kleim, J.P.8
Rosner, M.9
Hughes, S.H.10
Arnold, E.11
-
35
-
-
0035965124
-
Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation nonnucleoside inhibitors
-
Ren, J.; Nichols, C.; Bird, L.; Chamberlain, P.; Weaver, K.; Short, S.; Stuart, D. I.; Stammers, D. K. Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation nonnucleoside inhibitors. J. Mol. Biol. 2001, 372, 795-809.
-
(2001)
J. Mol. Biol.
, vol.372
, pp. 795-809
-
-
Ren, J.1
Nichols, C.2
Bird, L.3
Chamberlain, P.4
Weaver, K.5
Short, S.6
Stuart, D.I.7
Stammers, D.K.8
-
36
-
-
0036229823
-
Structural basis for the inhibitory efficacy of efavirenz (DMP-266), MSC194 and PNU142721 towards the HIV-1 RT K103N mutant
-
Lindberg, J.; Sigurdsson, S.; Lowgren, S.; Andersson, H. O.; Sahlberg, C.; Noreen, R.; Fridborg, K.; Zhang, H.; Unge, T. Structural basis for the inhibitory efficacy of efavirenz (DMP-266), MSC194 and PNU142721 towards the HIV-1 RT K103N mutant. Eur. J. Biochem. 2002, 269, 1670-1677.
-
(2002)
Eur. J. Biochem.
, vol.269
, pp. 1670-1677
-
-
Lindberg, J.1
Sigurdsson, S.2
Lowgren, S.3
Andersson, H.O.4
Sahlberg, C.5
Noreen, R.6
Fridborg, K.7
Zhang, H.8
Unge, T.9
-
37
-
-
2342620790
-
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related nonnucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants
-
Das, K.; Clark, A. D., Jr.; Lewi, P. J.; Heeres, J.; De Jonge, M. R.; Koymans, L. M.; Vinkers, H. M.; Daeyaert, F.; Ludovici, D. W.; Kukla, M. J.; De Corte, B.; Kavash, R. W.; Ho, C. Y.; Ye, H.; Lichtenstein, M. A.; Andries, K.; Pauwels R.; De Béthune, M.-P.; Boyer, P. L.; Clark, P.; Hughes, S. H.; Janssen, P. A.; Arnold, E. Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related nonnucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants. J. Med. Chem. 2004, 47, 2550-2560.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 2550-2560
-
-
Das, K.1
Clark Jr., A.D.2
Lewi, P.J.3
Heeres, J.4
De Jonge, M.R.5
Koymans, L.M.6
Vinkers, H.M.7
Daeyaert, F.8
Ludovici, D.W.9
Kukla, M.J.10
De Corte, B.11
Kavash, R.W.12
Ho, C.Y.13
Ye, H.14
Lichtenstein, M.A.15
Andries, K.16
Pauwels, R.17
De Béthune, M.-P.18
Boyer, P.L.19
Clark, P.20
Hughes, S.H.21
Janssen, P.A.22
Arnold, E.23
more..
-
38
-
-
10744233372
-
On the dectection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data
-
Lewi, P. J.; de Jonge, M.; Daeyaert, F.; Koymans, L.; Vinkers, M.; Heeres, J.; Janssen, P. A. J.; Arnold, E.; Das, K.; Clark, A. D., Jr.; Hughes, S. H.; Boyer, P. L.; de Béthune, M.-P.; Pauwels, R.; Andries, K.; Kukla, M.; Ludovici, D.; De Corte, B.; Kavash, R.; Ho, C. On the dectection of multiple-binding modes of ligands to proteins, from biological, structural, and modeling data. J. Comput. Aid. Des. 2003, 17, 129-134.
-
(2003)
J. Comput. Aid. Des.
, vol.17
, pp. 129-134
-
-
Lewi, P.J.1
De Jonge, M.2
Daeyaert, F.3
Koymans, L.4
Vinkers, M.5
Heeres, J.6
Janssen, P.A.J.7
Arnold, E.8
Das, K.9
Clark Jr., A.D.10
Hughes, S.H.11
Boyer, P.L.12
De Béthune, M.-P.13
Pauwels, R.14
Andries, K.15
Kukla, M.16
Ludovici, D.17
De Corte, B.18
Kavash, R.19
Ho, C.20
more..
-
39
-
-
0037571112
-
Merck molecular force field: I. Basis, form, scope, parametrization and performance of MMFF94
-
Halgren, T. A. Merck molecular force field: I. Basis, form, scope, parametrization and performance of MMFF94. J. Comput. Chem. 1998, 17, 490-519.
-
(1998)
J. Comput. Chem.
, vol.17
, pp. 490-519
-
-
Halgren, T.A.1
-
40
-
-
0023687234
-
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds
-
Pauwels, R.; Balzarini, J.; Baba, M.; Snoeck, R.; Schols, D.; Herdewijn, P.; Desmyter, J.; De Clercq, E. Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. J. Virol. Methods 1988, 20, 309-321.
-
(1988)
J. Virol. Methods
, vol.20
, pp. 309-321
-
-
Pauwels, R.1
Balzarini, J.2
Baba, M.3
Snoeck, R.4
Schols, D.5
Herdewijn, P.6
Desmyter, J.7
De Clercq, E.8
-
41
-
-
17944374798
-
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues
-
Ludovici, D. W.; De Corte, B. L.; Kukla, M. J.; Ye, H.; Ho, C. Y.; Lichtenstein, M. A.; Kavash, R. W.; Andries, K.; de Béthune, M.-P.; Azijn, H.; Pauwels, R.; Lewi, P. J.; Heeres, J.; Koymans, L. M.; de Jonge, M. R.; Van Aken, K. J.; Daeyaert, F. F.; Das, K.; Arnold E.; Janssen P. A. J. Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. Bioorg. Med. Chem. Lett. 2001, 11, 2235-2239.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2235-2239
-
-
Ludovici, D.W.1
De Corte, B.L.2
Kukla, M.J.3
Ye, H.4
Ho, C.Y.5
Lichtenstein, M.A.6
Kavash, R.W.7
Andries, K.8
De Béthune, M.-P.9
Azijn, H.10
Pauwels, R.11
Lewi, P.J.12
Heeres, J.13
Koymans, L.M.14
De Jonge, M.R.15
Van Aken, K.J.16
Daeyaert, F.F.17
Das, K.18
Arnold, E.19
Janssen, P.A.J.20
more..
-
42
-
-
7244229886
-
Correlations between Factors Determining the pharmacokinetics and Antiviral Activity of HIV-1 nonnucleoside reverse transcriptase inhibitors of the Diaryltriazine and Diarylpyrimidine classes of compounds
-
Lewi, P.; Arnold, E.; Andries, K.; Bohets, H.; Borghys H.; Clark, A. D., Jr.; Daeyaert F.; Das, K.; de Béthune M.-P.; de Jonge, M.; Heeres, J.; Koymans, L.; Leempoels, J.; Peeters, J.; Timmerman, Ph.; Van den Broeck, W.; Vanhoutte, F.; van't Klooster, G.; Vinkers, M.; Volovik, Y.; Janssen, P. A. J. Correlations between Factors Determining the pharmacokinetics and Antiviral Activity of HIV-1 nonnucleoside reverse transcriptase inhibitors of the Diaryltriazine and Diarylpyrimidine classes of compounds. Drugs R & D 2004, 5, 245-257.
-
(2004)
Drugs R & D
, vol.5
, pp. 245-257
-
-
Lewi, P.1
Arnold, E.2
Andries, K.3
Bohets, H.4
Borghys, H.5
Clark Jr., A.D.6
Daeyaert, F.7
Das, K.8
De Béthune, M.-P.9
De Jonge, M.10
Heeres, J.11
Koymans, L.12
Leempoels, J.13
Peeters, J.14
Timmerman, Ph.15
Van Den Broeck, W.16
Vanhoutte, F.17
Van't Klooster, G.18
Vinkers, M.19
Volovik, Y.20
Janssen, P.A.J.21
more..
-
43
-
-
15444361883
-
Concentration and pH dependence of aggregation of hydrophobic drug molecules and relevance to oral bioavailability
-
in press
-
Volovik Frenkel, Y.; Clark, A. D., Jr.; Das, K.; Wang, Y.; Lewi, P. J.; Janssen, P. A. J.; Arnold, E. Concentration and pH dependence of aggregation of hydrophobic drug molecules and relevance to oral bioavailability. J. Med. Chem., in press.
-
J. Med. Chem.
-
-
Volovik Frenkel, Y.1
Clark Jr., A.D.2
Das, K.3
Wang, Y.4
Lewi, P.J.5
Janssen, P.A.J.6
Arnold, E.7
-
44
-
-
0141923641
-
Identification and prediction of promiscuous aggregating inhibitors among known drugs
-
Seidler, J.; McGovern, S. L.; Doman, T. N.; Shoichet, B. K. Identification and prediction of promiscuous aggregating inhibitors among known drugs. J. Med. Chem. 2003, 46, 4477-4486.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4477-4486
-
-
Seidler, J.1
McGovern, S.L.2
Doman, T.N.3
Shoichet, B.K.4
-
45
-
-
0141792701
-
A specific mechanism of nonspecific inhibition
-
McGovern, S. L.; Helfand, B. T.; Feng, B.; Shoichet, B. K. A specific mechanism of nonspecific inhibition. J. Med. Chem. 2003, 46, 4265-4272.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4265-4272
-
-
McGovern, S.L.1
Helfand, B.T.2
Feng, B.3
Shoichet, B.K.4
-
47
-
-
0035523263
-
Strategies for drug screening in drug discovery and development
-
Bohets, H.; Annaert, P.; Mannens, G.; van Beijsterveldt, L.; Anciaux, K.; Verboven, P.; Meuldermans, W.; Lavrijsen K. Strategies for drug screening in drug discovery and development. Curr. Top. Med. Chem. 2001, 1, 367-383.
-
(2001)
Curr. Top. Med. Chem.
, vol.1
, pp. 367-383
-
-
Bohets, H.1
Annaert, P.2
Mannens, G.3
Van Beijsterveldt, L.4
Anciaux, K.5
Verboven, P.6
Meuldermans, W.7
Lavrijsen, K.8
-
48
-
-
0032403490
-
Physiological considerations in the design of particulate dosage forms for oral vaccine delivery
-
Yeh, P.-Y.; Ellens, H.; Smith, P. L. Physiological considerations in the design of particulate dosage forms for oral vaccine delivery. Adv. Drug Deliv. Rev. 1998, 34, 123-133.
-
(1998)
Adv. Drug Deliv. Rev.
, vol.34
, pp. 123-133
-
-
Yeh, P.-Y.1
Ellens, H.2
Smith, P.L.3
-
49
-
-
0001684418
-
Distribution of vitamin A in tissues as visualized by fluorescence microscopy
-
Popper, H. Distribution of vitamin A in tissues as visualized by fluorescence microscopy. Physiol. Rev. 1944, 24, 205-224.
-
(1944)
Physiol. Rev.
, vol.24
, pp. 205-224
-
-
Popper, H.1
-
52
-
-
9644291579
-
TMC125, a novel next generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant HIV-1
-
in press
-
Andries, K.; Azijn, H.; Thielemans, T.; Ludovici, D.; Kukla, M.; Heeres, J.; Janssen, P.(+); De Corte, B.; Pauwels, R.; de Béthune, M.-P. TMC125, a novel next generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant HIV-1. AACN Clin. Issues 2004, in press
-
(2004)
AACN Clin. Issues
-
-
Andries, K.1
Azijn, H.2
Thielemans, T.3
Ludovici, D.4
Kukla, M.5
Heeres, J.6
Janssen, P.7
De Corte, B.8
Pauwels, R.9
De Béthune, M.-P.10
-
53
-
-
0023199690
-
Guide for performing the mouse lymphoma assay for mammalian cell mutagenicity
-
Clive, D.; Caspary, W.; Kirby, P.; Krehl. R.; Moore, M.; Mayo, J.; Oberly, T. J. Guide for performing the mouse lymphoma assay for mammalian cell mutagenicity. Mutation Res. 1987, 189, 143-156.
-
(1987)
Mutation Res.
, vol.189
, pp. 143-156
-
-
Clive, D.1
Caspary, W.2
Kirby, P.3
Krehl, R.4
Moore, M.5
Mayo, J.6
Oberly, T.J.7
-
54
-
-
15444378783
-
-
Annex to the Commission Directive 92/69 EEC, adapting Council Directive 67/548/EEC, July 31
-
EEC test method B. 12. Micronucleus test. Annex to the Commission Directive 92/69 EEC, adapting Council Directive 67/548/EEC, July 31, 1992
-
(1992)
EEC Test Method B. 12. Micronucleus Test
-
-
-
56
-
-
0018623097
-
A chronically implantable catheter-tip micromanometer (JSI 0400) that can be calibrated after implantation
-
Smet, F.; D'Aubioul, J.; van Gerven, W.; Xhonneux, R.; Reneman, RS. A chronically implantable catheter-tip micromanometer (JSI 0400) that can be calibrated after implantation. Cardiovasc. Res. 1979, 13, 601-605.
-
(1979)
Cardiovasc. Res.
, vol.13
, pp. 601-605
-
-
Smet, F.1
D'Aubioul, J.2
Van Gerven, W.3
Xhonneux, R.4
Reneman, R.S.5
-
57
-
-
0022540388
-
Reference range database for serum chemistry and hematology values in laboratory animals
-
Wolford, S. T.; Schroer, R. A.; Gohs, F. X.; Gallo, P. P.; Brodeck, M.; Falk, H. B.; Ruhren, R. Reference range database for serum chemistry and hematology values in laboratory animals. J. Toxicol. Environ. Health 1986, 18, 161-88.
-
(1986)
J. Toxicol. Environ. Health
, vol.18
, pp. 161-188
-
-
Wolford, S.T.1
Schroer, R.A.2
Gohs, F.X.3
Gallo, P.P.4
Brodeck, M.5
Falk, H.B.6
Ruhren, R.7
-
59
-
-
0001513406
-
International Conference on Harmonisation: Guidelines on the Assessment of Systemic Exposure in Toxicity Studies
-
International Conference on Harmonisation: Guidelines on the Assessment of Systemic Exposure in Toxicity Studies. FDA, Fed. Regist. 1995, 60, 11264-11268.
-
(1995)
FDA, Fed. Regist.
, vol.60
, pp. 11264-11268
-
-
-
60
-
-
20144362135
-
Synthesis of novel diarylpyrimidine (DAPY) analogues and their antiviral activity against HIV-1
-
in press
-
Guillemont, J.; Pasquier, E.; Palandjian, P.; Vernier, D.; Gaurrand, S.; Lewi, P. J.; Heeres, J.; de Jonge, M. R.; Koymans, L. M. H.; Daeyaert, F. F. D.; Vinkers, M. H.; Arnold, E.; Das, K.; Pauwels, R.; Andries, K.; de Béthune, M.-P.; Bettens, E.; Hertogs, K.; Wigerinck, P.; Timmerman, P.; Janssen, P. A. J. Synthesis of novel diarylpyrimidine (DAPY) analogues and their antiviral activity against HIV-1. J. Med. Chem., in press.
-
J. Med. Chem.
-
-
Guillemont, J.1
Pasquier, E.2
Palandjian, P.3
Vernier, D.4
Gaurrand, S.5
Lewi, P.J.6
Heeres, J.7
De Jonge, M.R.8
Koymans, L.M.H.9
Daeyaert, F.F.D.10
Vinkers, M.H.11
Arnold, E.12
Das, K.13
Pauwels, R.14
Andries, K.15
De Béthune, M.-P.16
Bettens, E.17
Hertogs, K.18
Wigerinck, P.19
Timmerman, P.20
Janssen, P.A.J.21
more..
|