-
1
-
-
0020596551
-
Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS)
-
Barre-Sinoussi F, Chermann JC, Rey F, et al. Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS). Science 1983;220:868-71 (Pubitemid 13080157)
-
(1983)
Science
, vol.220
, Issue.4599
, pp. 868-871
-
-
Barre Sinoussi, F.1
Chermann, J.C.2
Rey, F.3
-
3
-
-
0030018156
-
CC CKR5: A RANTES, MIP-1α, MIP-1β receptor as a fusion cofactor for macrophage-tropic HIV-1
-
Alkhatib G, Combadiere C, Broder CC, et al. CC CKRS: A RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1. Science 1996;272:1955-8 (Pubitemid 26234510)
-
(1996)
Science
, vol.272
, Issue.5270
, pp. 1955-1958
-
-
Alkhatib, G.1
Combadiere, C.2
Broder, C.C.3
Feng, Y.4
Kennedy, P.E.5
Murphy, P.M.6
Berger, E.A.7
-
4
-
-
0005014748
-
The β-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates
-
DOI 10.1016/S0092-8674(00)81313-6
-
Choe H, Farzan M, Sun Y, et al. The beta-chemokine receptors CCR3 and CCR5 facilitate infection by primary HIV-1 isolates. Cell 1996;6:1135-48 (Pubitemid 26231178)
-
(1996)
Cell
, vol.85
, Issue.7
, pp. 1135-1148
-
-
Choe, H.1
Farzan, M.2
Sun, Y.3
Sullivan, N.4
Rollins, B.5
Ponath, P.D.6
Wu, L.7
Mackay, C.R.8
LaRosa, G.9
Newman, W.10
Gerard, N.11
Gerard, C.12
Sodroski, J.13
-
5
-
-
15844419153
-
Identification of a major co-receptor for primary isolates of HIV-1
-
DOI 10.1038/381661a0
-
Deng HK, Liu R, Ellmeier W, et al. Identification of a major co-receptor for primary isolates of HIV-1. Nature 1996;381:661-6 (Pubitemid 26197679)
-
(1996)
Nature
, vol.381
, Issue.6584
, pp. 661-666
-
-
Deng, H.1
Liu, R.2
Ellmeier, W.3
Choe, S.4
Unutmaz, D.5
Burkhart, M.6
Di Marzio, P.7
Marmon, S.8
Sutton, R.E.9
Mark Hill, C.10
Davis, C.B.11
Peiper, S.C.12
Schall, T.J.13
Littman, D.R.14
Landau, N.R.15
-
6
-
-
0030604727
-
A dual-tropic primary HIV-1 isolate that uses fusin and the β-chemokine receptors CKR-5, CKR-3, and CKR-2b as fusion cofactors
-
DOI 10.1016/S0092-8674(00)81314-8
-
Doranz BJ, Rucker J, Yi YJ, et al. A dual-tropic primary HIV-1 isolate that uses fusin and the beta-chemokine receptors CKR-5, CKR-3, and CKR-2b as fusion cofactors. Cell 1996;85:1149-58 (Pubitemid 26235280)
-
(1996)
Cell
, vol.85
, Issue.7
, pp. 1149-1158
-
-
Doranz, B.J.1
Rucker, J.2
Yi, Y.3
Smyth, R.J.4
Samson, M.5
Peiper, S.C.6
Parmentier, M.7
Collman, R.G.8
Doms, R.W.9
-
7
-
-
15844389650
-
+ cells is mediated by the chemokine receptor CC-CKR-5
-
DOI 10.1038/381667a0
-
Dragic T, Litwin V, Allaway GP, et al. HIV-1 entry into CD4(+) cells is mediated by the chemokine receptor CC-CKR-5. Nature 1996;381:667-73 (Pubitemid 26197680)
-
(1996)
Nature
, vol.381
, Issue.6584
, pp. 667-673
-
-
Dragic, T.1
Litwin, V.2
Allaway, G.P.3
Martin, S.R.4
Huang, Y.5
Nagashima, K.A.6
Cayanan, C.7
Maddon, P.J.8
Koup, R.A.9
Moore, J.P.10
Paxton, W.A.11
-
8
-
-
0030002637
-
HIV-1 entry cofactor: Functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor
-
Feng Y, Broder CC, Kennedy PE, Berger EA. HIV-1 entry cofactor: Functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science 1996;272:872-7 (Pubitemid 26154590)
-
(1996)
Science
, vol.272
, Issue.5263
, pp. 872-877
-
-
Feng, Y.1
Broder, C.C.2
Kennedy, P.E.3
Berger, E.A.4
-
9
-
-
0032577550
-
HIV entry and its inhibition
-
DOI 10.1016/S0092-8674(00)81430-0
-
Chan DC, Kim PS. HIV entry and its inhibition. Cell 1998;93:681-4 (Pubitemid 28257575)
-
(1998)
Cell
, vol.93
, Issue.5
, pp. 681-684
-
-
Chan, D.C.1
Kim, P.S.2
-
10
-
-
0027692502
-
A synthetic peptide from HIV-1 gp41 is a potent inhibitor of virus-mediated cell-cell fusion
-
The discovery of a fusion inhibitor Enfuvirtide
-
Wild CT, Greenwell TK, Matthews TJ, et al. A synthetic peptide from HIV-1 gp41 is a potent inhibitor of virus-mediated cell-cell fusion. AIDS Res Hum Retroviruses 1993;9:1051-3. The discovery of a fusion inhibitor Enfuvirtide.
-
(1993)
AIDS Res Hum Retroviruses
, vol.9
, pp. 1051-1053
-
-
Wild, C.T.1
Greenwell, T.K.2
Matthews, T.J.3
-
11
-
-
15344350690
-
Species differences in the disposition of the CCR5 antagonist, UK-427,857, a new potential treatment for HIV
-
DOI 10.1124/dmd.104.002626
-
Walker DK, Abel S, Comby P, et al. Species differences in the disposition of the CCR5 antagonist, UK-427,857, a new potential treatment for HIV. Drug Metab Dispos 2005;33:587-95. The discovery of an entry inhibitor Maraviroc (CCR5 antagonist). (Pubitemid 40393203)
-
(2005)
Drug Metabolism and Disposition
, vol.33
, Issue.4
, pp. 587-595
-
-
Walker, D.K.1
Abel, S.2
Comby, P.3
Muirhead, G.J.4
Nedderman, A.N.R.5
Smith, D.A.6
-
12
-
-
34147116231
-
Raltegravir: A new antiretroviral class for salvage therapy
-
The discovery of an integrase inhibitor Raltegravir
-
Cahn P, Sued O. Raltegravir: A new antiretroviral class for salvage therapy. Lancet 2007;369:1235-6. The discovery of an integrase inhibitor Raltegravir.
-
(2007)
Lancet
, vol.369
, pp. 1235-1036
-
-
Cahn, P.1
Sued, O.2
-
13
-
-
34147136222
-
Safety and efficacy of the HIV-1 integrase inhibitor Raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: A phase II randomised controlled trial
-
The discovery of an integrase inhibitor Raltegravir
-
Grinsztejn B, Nguyen B-Y, Katlama C, et al. Safety and efficacy of the HIV-1 integrase inhibitor Raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: A phase II randomised controlled trial. Lancet 2007;369:1261-9. The discovery of an integrase inhibitor Raltegravir.
-
(2007)
Lancet
, vol.369
, pp. 1261-1369
-
-
Grinsztejn, B.1
Nguyen, B-.Y.2
Katlama, C.3
-
14
-
-
0028834461
-
A trimeric structural domain of the HIV-1 transmembrane glycoprotein
-
Lu M, Blacklow SC, Kim PS. A trimeric structural domain of the HIV-1 transmembrane glycoprotein. Nat Struct Biol 1995;2:1075-82
-
(1995)
Nat Struct Biol
, vol.2
, pp. 1075-1082
-
-
Lu, M.1
Blacklow, S.C.2
Kim, P.S.3
-
15
-
-
78649842313
-
Resistance profiles of novel electrostatically constrained HIV-1 fusion inhibitors
-
Shimura K, Nameki D, Kajiwara K, et al. Resistance profiles of novel electrostatically constrained HIV-1 fusion inhibitors. J Biol Chem 2010;285:39471-80
-
(2010)
J Biol Chem
, vol.285
, pp. 39471-39480
-
-
Shimura, K.1
Nameki, D.2
Kajiwara, K.3
-
16
-
-
0030970693
-
Core structure of gp41 from the HIV envelope glycoprotein
-
Chan DC, Fass D, Berger JM, Kim PS. Core structure of gp41 from the HIV envelope glycoprotein. Cell 1997;89:263-73 (Pubitemid 27199898)
-
(1997)
Cell
, vol.89
, Issue.2
, pp. 263-273
-
-
Chan, D.C.1
Fass, D.2
Berger, J.M.3
Kim, P.S.4
-
17
-
-
0037119022
-
Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells
-
Otaka A, Nakamura M, Nameki D, et al. Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells. Angew Chem Int Ed 2022;41:2937-40
-
(2022)
Angew Chem Int Ed
, vol.41
, pp. 2937-2940
-
-
Otaka, A.1
Nakamura, M.2
Nameki, D.3
-
18
-
-
59649099932
-
Electrostatically constrained alpha-helical peptide inhibits replication of HIV-1 resistant to Enfuvirtide
-
Nishikawa H, Nakamura S, Kodama E, et al. Electrostatically constrained alpha-helical peptide inhibits replication of HIV-1 resistant to Enfuvirtide. Int J Biochem Cell Biol 2009;41:891-9
-
(2009)
Int J Biochem Cell Biol
, vol.41
, pp. 891-899
-
-
Nishikawa, H.1
Nakamura, S.2
Kodama, E.3
-
19
-
-
15744393651
-
Different from the HIV fusion inhibitor C34, the anti-HIV drug fuzeon (T-20) inhibits HIV-1 entry by targeting multiple sites in gp41 and gp120
-
DOI 10.1074/jbc.M411141200
-
Liu S, Lu H, Xu Y, et al. Different from the HIV fusion inhibitor C34, the anti-HIV drug fuzeon (T-20) inhibits HIV-1 entry by targeting multiple sites in gp41 and gp120. J Biol Chem 2005;280:11259-73. (Pubitemid 40418432)
-
(2005)
Journal of Biological Chemistry
, vol.280
, Issue.12
, pp. 11259-11273
-
-
Liu, S.1
Lu, H.2
Niu, J.3
Xu, Y.4
Wu, S.5
Jiang, S.6
-
20
-
-
0034890660
-
Sensitivity of human immunodeficiency virus type 1 to fusion inhibitors targeted to the gp41 first heptad repeat involves distinct regions of gp41 and is consistently modulated by gp120 interactions with the coreceptor
-
DOI 10.1128/JVI.75.18.8605-8614.2001
-
Derdeyn CA, Decker JM, Sfakianos JN, et al. Sensitivity of human immunodeficiency virus type 1 to fusion inhibitors targeted to the gp41 first heptad repeat involves distinct regions of gp41 and is consistently modulated by gp120 interactions with the coreceptor. J Virol 2001;75:8605-14 (Pubitemid 32768965)
-
(2001)
Journal of Virology
, vol.75
, Issue.18
, pp. 8605-8614
-
-
Derdeyn, C.A.1
Decker, J.M.2
Sfakianos, J.N.3
Zhang, Z.4
O'Brien, W.A.5
Ratner, L.6
Shaw, G.M.7
Hunter, E.8
-
21
-
-
8844228894
-
HIV fusion inhibitor peptide T-1249 is able to insert or adsorb to lipidic bilayers. Putative correlation with improved efficiency
-
DOI 10.1021/ja0459882
-
Veiga AS, Santos NC, Loura LM, et al. HIV fusion inhibitor peptide T-1249 is able to insert or adsorb to lipidic bilayers. Putative correlation with improved efficiency. J Am Chem Soc 2004;126:14758-63. The discovery of a fusion inhibitor T-1249, a follow-on to Enfuvirtide. (Pubitemid 39532156)
-
(2004)
Journal of the American Chemical Society
, vol.126
, Issue.45
, pp. 14758-14763
-
-
Veiga, A.S.1
Santos, N.C.2
Loura, L.M.S.3
Fedorov, A.4
Castanho, M.A.R.B.5
-
22
-
-
3042799382
-
Prospects of HIV-1 entry inhibitors as novel therapeutics
-
DOI 10.1002/rmv.435
-
Pierson TC, Doms RW, Pohlmann S. Prospects of HIV-1 entry inhibitors as novel therapeutics. Rev Med Virol 2004;14:255-70 (Pubitemid 38879817)
-
(2004)
Reviews in Medical Virology
, vol.14
, Issue.4
, pp. 255-270
-
-
Pierson, T.C.1
Doms, R.W.2
Pohlmann, S.3
-
23
-
-
2442511737
-
High throughput screening and characterization of HIV-1 entry inhibitors targeting gp41: Theories and techniques
-
DOI 10.2174/1381612043384466
-
Liu S, Jiang S. High throughput screening and characterization of HIV-1 entry inhibitors targeting gp41: Theories and techniques. Curr Pharm Des 2004;10:1827-43 (Pubitemid 38647464)
-
(2004)
Current Pharmaceutical Design
, vol.10
, Issue.15
, pp. 1827-1843
-
-
Liu, S.1
Jiang, S.2
-
24
-
-
11144358392
-
Small-molecule inhibitors of HIV-1 entry block receptor-induced conformational changes in the viral envelope glycoproteins
-
DOI 10.1073/pnas.0307953101
-
Si Z, Madani N, Cox JM, et al. Small-molecule inhibitors of HIV-1 entry block receptor-induced conformational changes in the viral envelope glycoproteins. Proc Natl Acad Sci USA 2004;101:5036-41 (Pubitemid 38469198)
-
(2004)
Proceedings of the National Academy of Sciences of the United States of America
, vol.101
, Issue.14
, pp. 5036-5041
-
-
Si, Z.1
Madani, N.2
Cox, J.M.3
Chruma, J.J.4
Klein, J.C.5
Schon, A.6
Phan, N.7
Wang, L.8
Biorn, A.C.9
Cocklin, S.10
Chaiken, I.11
Freire, E.12
Smith III, A.B.13
Sodroski, J.G.14
-
25
-
-
0032876381
-
Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial libraries of non-natural binding elements
-
DOI 10.1038/13324
-
Ferrer M, Kapoor TM, Strassmaier T, et al. Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial libraries of non-natural binding elements. Nat Struct Biol 1999;6:953-60 (Pubitemid 29463310)
-
(1999)
Nature Structural Biology
, vol.6
, Issue.10
, pp. 953-960
-
-
Ferrer, M.1
Kapoor, T.M.2
Strassmaier, T.3
Weissenhorn, W.4
Skehel, J.J.5
Oprian, D.6
Schreiber, S.L.7
Wiley, D.C.8
Harrison, S.C.9
-
26
-
-
77951287748
-
Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies
-
The development of an HIV vaccine based on trimer mimic of the gp41 HR1 region
-
Nakahara T, Nomura W, Ohba K, et al. Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies. Bioconjug Chem 2010;21:709-14. The development of an HIV vaccine based on trimer mimic of the gp41 HR1 region.
-
(2010)
Bioconjug Chem
, vol.21
, pp. 709-714
-
-
Nakahara, T.1
Nomura, W.2
Ohba, K.3
-
28
-
-
0033012398
-
Chemokine receptors as HIV-1 coreceptors: Roles in viral entry, tropism, and disease
-
DOI 10.1146/annurev.immunol.17.1.657
-
Berger EA, Murphy PM, Farber JM. Chemokine receptors as HIV-1 coreceptors: Roles in viral entry, tropism, and disease. Annu Rev Immunol 1999;14:657-700 (Pubitemid 29241137)
-
(1999)
Annual Review of Immunology
, vol.17
, pp. 657-700
-
-
Berger, E.A.1
Murphy, P.M.2
Farber, J.M.3
-
29
-
-
40549102421
-
Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects
-
DOI 10.1111/j.1365-2125.2008.03137.x
-
Abel S, Russell D, Whitlock LA, et al. Assessment of the absorption, metabolism and absolute bioavailability of Maraviroc in healthy male subjects. Br J Clin Pharmacol 2008;65:60-7 (Pubitemid 351366540)
-
(2008)
British Journal of Clinical Pharmacology
, vol.65
, Issue.SUPPL. 1
, pp. 60-67
-
-
Abel, S.1
Russell, D.2
Whitlock, L.A.3
Ridgway, C.E.4
Nedderman, A.N.R.5
Walker, D.K.6
-
30
-
-
40549106758
-
A population pharmacokinetic meta-analysis of maraviroc in healthy volunteers and asymptomatic HIV-infected subjects
-
DOI 10.1111/j.1365-2125.2008.03139.x
-
Chan PLS, Weatherley B, McFadyen L, et al. A population pharmacokinetic meta-analysis of Maraviroc in healthy volunteers and asymptomatic HIV-infected subjects. Br J Clin Pharmacol 2008;65:76-85 (Pubitemid 351366542)
-
(2008)
British Journal of Clinical Pharmacology
, vol.65
, Issue.SUPPL. 1
, pp. 76-85
-
-
Chan, P.L.S.1
Weatherley, B.2
McFadyen, L.3
-
31
-
-
78651075863
-
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: The discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2- methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1] oct-8-yl]propyl} acetamide (PF-232798)
-
Stupple PA, Batchelor DV, Corless M, et al. An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: The discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6, 7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl} acetamide (PF-232798). J Med Chem 2011;54:67-77
-
(2011)
J Med Chem
, vol.54
, pp. 67-77
-
-
Stupple, P.A.1
Batchelor, D.V.2
Corless, M.3
-
32
-
-
13044256383
-
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
-
DOI 10.1073/pnas.96.10.5698
-
Baba M, Nishimura O, Kanzaki N, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci USA 1999;96:5698-703 (Pubitemid 29234681)
-
(1999)
Proceedings of the National Academy of Sciences of the United States of America
, vol.96
, Issue.10
, 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
-
33
-
-
0034117636
-
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: Synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety
-
DOI 10.1021/jm9906264
-
Shiraishi M, Aramaki Y, Seto M, et al. Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: Synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. J Med Chem 2000;43:2049-63 (Pubitemid 30340944)
-
(2000)
Journal of Medicinal Chemistry
, vol.43
, Issue.10
, pp. 2049-2063
-
-
Shiraishi, M.1
Aramaki, Y.2
Seto, M.3
Imoto, H.4
Nishikawa, Y.5
Kanzaki, N.6
Okamoto, M.7
Sawada, H.8
Nishimura, O.9
Baba, M.10
Fujino, M.11
-
34
-
-
2542534321
-
CCR5 antagonists as anti-HIV-1 agents. 1. Synthesis and biological evaluation of 5-oxopyrrolidine-3-carboxamide derivatives
-
DOI 10.1248/cpb.52.63
-
Imamura S, Ishihara Y, Hattori T, et al. CCR5 antagonists as anti-HIV-1 agents. 1. Synthesis and biological evaluation of 5-oxopyrrolidine-3-carboxamide derivatives. Chem Pharm Bull 2004;52:63-73 (Pubitemid 41685553)
-
(2004)
Chemical and Pharmaceutical Bulletin
, vol.52
, Issue.1
, pp. 63-73
-
-
Imamura, S.1
Ishihara, Y.2
Hattori, T.3
Kurasawa, O.4
Matsushita, Y.5
Sugihara, Y.6
Kanzaki, N.7
Iizawa, Y.8
Baba, M.9
Hashiguchi, S.10
-
35
-
-
33646460235
-
Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent anti-HIV-1 activity
-
Imamura S, Ichikawa T, Nishikawa Y, et al. Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent anti-HIV-1 activity. J Med Chem 2006;49:2784-93
-
(2006)
J Med Chem
, vol.49
, pp. 2784-2793
-
-
Imamura, S.1
Ichikawa, T.2
Nishikawa, Y.3
-
36
-
-
2342544143
-
Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl) carbonyl]-4-[4-{2-methoxy-1(R)-4- (trifluoromethyl)-phenyl}ethyl-3(S) -methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist
-
DOI 10.1021/jm0304515
-
Tagat JR, McCombie SW, Nazareno DV, et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5- pyrimidinyl)carbonyl]-4-[4-{2-methoxy-1 (R)-4-(trifluoromethyl)-phenyl}ethyl- 3(S)-methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonists. J Med Chem 2003;47:2405-8 (Pubitemid 38580075)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.10
, pp. 2405-2408
-
-
Tagat, J.R.1
McCombie, S.W.2
Nazareno, D.3
Labroli, M.A.4
Xiao, Y.5
Steensma, R.W.6
Strizki, J.M.7
Baroudy, B.M.8
Cox, K.9
Lachowicz, J.10
Varty, G.11
Watkins, R.12
-
37
-
-
54749134143
-
Phase II study of vicriviroc versus efavirenz (both with zidovudine/lamivudine) in treatment-naive subjects with HIV-1 infection
-
Landovitz RJ, Angel JB, Hoffmann C, et al. Phase II study of vicriviroc versus efavirenz (both with zidovudine/lamivudine) in treatment-naive subjects with HIV-1 infection. J Infect Dis 2008;198:1113-22
-
(2008)
J Infect Dis
, vol.198
, pp. 1113-1122
-
-
Landovitz, R.J.1
Angel, J.B.2
Hoffmann, C.3
-
38
-
-
77954974723
-
Phase 3 trials of Vicriviroc in treatment-experienced subjects demonstrate safety but not significantly superior efficacy over potent background regimens
-
16-19 February; San Francisco CA
-
Gathe J, Diaz R, Fatkenheuer G, et al. Phase 3 trials of Vicriviroc in treatment-experienced subjects demonstrate safety but not significantly superior efficacy over potent background regimens. 17th CROI Conference on Retroviruses and Opportunistic Infections; 16-19 February 2010; San Francisco CA
-
(2010)
17th CROI Conference on Retroviruses and Opportunistic Infections
-
-
Gathe, J.1
Diaz, R.2
Fatkenheuer, G.3
-
39
-
-
33745807624
-
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists
-
DOI 10.1021/jm060051s
-
Habashita H, Kokubo M, Hamano S, et al. Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists. J Med Chem 2006;49:4140-52 (Pubitemid 44036659)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.14
, pp. 4140-4152
-
-
Habashita, H.1
Kokubo, M.2
Hamano, S.-I.3
Hamanaka, N.4
Toda, M.5
Shibayama, S.6
Tada, H.7
Sagawa, K.8
Fukushima, D.9
Maeda, K.10
Mitsuya, H.11
-
40
-
-
0035282432
-
Involvement of chemokine receptors in breast cancer metastasis
-
DOI 10.1038/35065016
-
Muller A, Homey B, Soto H, et al. Involvement of chemokine receptors in breast cancer metastasis. Nature 2001;410:50-6 (Pubitemid 32225831)
-
(2001)
Nature
, vol.410
, Issue.6824
, pp. 50-56
-
-
Muller, A.1
Homey, B.2
Soto, H.3
Ge, N.4
Catron, D.5
Buchanan, M.E.6
McClanahan, T.7
Murphy, E.8
Yuan, W.9
Wagner, S.N.10
Barrera, J.L.11
Mohar, A.12
Verastegui, E.13
Zlotnik, A.14
-
41
-
-
0142102523
-
T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer
-
DOI 10.1016/S0014-5793(03)00824-X
-
Tamamura H, Hori A, Kanzaki N, et al. T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer. FEBS Lett 2003;550:79-83 (Pubitemid 37281361)
-
(2003)
FEBS Letters
, vol.550
, Issue.1-3
, pp. 79-83
-
-
Tamamura, H.1
Hori, A.2
Kanzaki, N.3
Hiramatsu, K.4
Mizumoto, M.5
Nakashima, H.6
Yamamoto, N.7
Otaka, A.8
Fujii, N.9
-
42
-
-
2942654586
-
A single treatment with microcapsules containing a CXCR4 antagonist suppresses pulmonary metastasis of murine melanoma
-
DOI 10.1016/j.bbrc.2004.05.155, PII S0006291X04011301
-
Takenaga M, Tamamura H, Hiramatsu K, et al. A single treatment with microcapsules containing a CXCR4 antagonist suppresses pulmonary metastasis of murine melanoma. Biochem Biophys Res Commun 2004;320:226-32 (Pubitemid 38781805)
-
(2004)
Biochemical and Biophysical Research Communications
, vol.320
, Issue.1
, pp. 226-232
-
-
Takenaga, M.1
Tamamura, H.2
Hiramatsu, K.3
Nakamura, N.4
Yamaguchi, Y.5
Kitagawa, A.6
Kawai, S.7
Nakashima, H.8
Fujii, N.9
Igarashi, R.10
-
43
-
-
0036464610
-
Distinctive features of "nurselike" cells that differentiate in the context of chronic lymphocytic leukemia
-
DOI 10.1182/blood.V99.3.1030
-
Tsukada N, Burger JA, Zvaifler NJ, Kipps TJ. Distinctive features of "nurselike" cells that differentiate in thecontext of chronic lymphocytic leukemia. Blood 2002;99:1030-7 (Pubitemid 34525568)
-
(2002)
Blood
, vol.99
, Issue.3
, pp. 1030-1037
-
-
Tsukada, N.1
Burger, J.A.2
Zvaifler, N.J.3
Kipps, T.J.4
-
44
-
-
0038103869
-
Effects of inhibitors of the chemokine receptor CXCR4 on acute lymphoblastic leukemia cells in vitro
-
DOI 10.1038/sj.leu.2402998
-
Juarez J, Bradstock KF, Gottlieb DJ, Bendall LJ. Effects of inhibitors of the chemokine receptor CXCR4 on acute lymphoblastic leukemia cells in vitro. Leukemia 2003;17:1294-300 (Pubitemid 36857336)
-
(2003)
Leukemia
, vol.17
, Issue.7
, pp. 1294-1300
-
-
Juarez, J.1
Bradstock, K.F.2
Gottlieb, D.J.3
Bendall, L.J.4
-
45
-
-
0034544508
-
Stromal cell-derived factor-1-CXC chemokine receptor 4 interactions play a central role in CD4(+) T cell accumulation in rheumatoid arthritis synovium
-
Nanki T, Hayashida K, EI-Gabalawy HS, et al. Stromal cell-derived factor-1-CXC chemokine receptor 4 interactions play a central role in CD4(+) T cell accumulation in rheumatoid arthritis synovium. J Immunol 2000;165:6590-8
-
(2000)
J Immunol
, vol.165
, pp. 6590-6598
-
-
Nanki, T.1
Hayashida, K.2
El-Gabalawy, H.S.3
-
46
-
-
3042593906
-
Identification of a CXCR4 antagonist, a T140 analog, as an anti-rheumatoid arthritis agent
-
DOI 10.1016/j.febslet.2004.05.056, PII S0014579304006647
-
Tamamura H, Fujisawa M, Hiramatsu K, et al. Identification of a CXCR4 antagonist, a T140 analog, as an anti-rheumatoid arthritis agent. FEBS Lett 2004;569:99-104 (Pubitemid 38844600)
-
(2004)
FEBS Letters
, vol.569
, Issue.1-3
, pp. 99-104
-
-
Tamamura, H.1
Fujisawa, M.2
Hiramatsu, K.3
Mizumoto, M.4
Nakashima, H.5
Yamamoto, N.6
Otaka, A.7
Fujii, N.8
-
47
-
-
0032583575
-
A low-molecular-weight inhibitor against the chemokine receptor CXCR4: A strong anti-HIV peptide T140
-
DOI 10.1006/bbrc.1998.9871
-
Tamamura H, Xu Y, Hattori T, et al. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: A strong anti-HIV peptide T140. Biochem Biophys Res Commun 1998;253:877-82. The development of a peptidic CXCR4 antagonist T140. (Pubitemid 29039238)
-
(1998)
Biochemical and Biophysical Research Communications
, vol.253
, Issue.3
, pp. 877-882
-
-
Tamamura, H.1
Xu, Y.2
Hattori, T.3
Zhang, X.4
Arakaki, R.5
Kanbara, K.6
Omagari, A.7
Otaka, A.8
Ibuka, T.9
Yamamoto, N.10
Nakashima, H.11
Fujii, N.12
-
48
-
-
0142096799
-
Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives
-
Tamamura H, Hiramatsu K, Kusano S, et al. Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives. Org Biomol Chem 2003;1:3656-62
-
(2003)
Org Biomol Chem
, vol.1
, pp. 3656-3662
-
-
Tamamura, H.1
Hiramatsu, K.2
Kusano, S.3
-
49
-
-
0345412742
-
Enhancement of the T140-based pharmacophores leads to the development of more potent and bio-stable CXCR4 antagonists
-
The development of biostable derivatives of a CXCR4 antagonist T140
-
Tamamura H, Hiramatsu K, Mizumoto M, et al. Enhancement of the T140-based pharmacophores leads to the development of more potent and bio-stable CXCR4 antagonists. Org Biomol Chem 2003;1:3663-9. The development of biostable derivatives of a CXCR4 antagonist T140.
-
(2003)
Org Biomol Chem
, vol.1
, pp. 3663-3669
-
-
Tamamura, H.1
Hiramatsu, K.2
Mizumoto, M.3
-
50
-
-
10744227507
-
Molecular-size reduction of a potent CXCR4-chemokine antagonist using orthogonal combination of conformation- and sequence-based libraries
-
DOI 10.1002/anie.200351024
-
Fujii N, Oishi S, Hiramatsu K, et al. Molecular-size reduction of a potent CXCR4-chemokine antagonist using orthogonal combination of conformation-and sequence-based libraries. Angew Chem Int Ed 2003;42:3251-3 (Pubitemid 36917168)
-
(2003)
Angewandte Chemie - International Edition
, vol.42
, Issue.28
, pp. 3251-3253
-
-
Fujii, N.1
Oishi, S.2
Hiramatsu, K.3
Araki, T.4
Ueda, S.5
Tamamura, H.6
Otaka, A.7
Kusano, S.8
Terakubo, S.9
Nakashima, H.10
Broach, J.A.11
Trent, J.O.12
Wang, Z.-X.13
Peiper, S.C.14
-
51
-
-
0030830661
-
Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4
-
The development of a non-peptidic CXCR4 antagonist AMD3100
-
Schols D, Struyf S, Van Damme J, et al. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4. J Exp Med 1997;186:1383-8. The development of a non-peptidic CXCR4 antagonist AMD3100.
-
(1997)
J Exp Med
, vol.186
, pp. 1383-1398
-
-
Schols, D.1
Struyf, S.2
Van Damme, J.3
-
52
-
-
0038681342
-
The bicyclam AMD3100 story
-
DOI 10.1038/nrd1134
-
De Clercq E. The bicyclam AMD3100 story. Nat Rev Drug Discov 2003;2:581-7 (Pubitemid 37361749)
-
(2003)
Nature Reviews Drug Discovery
, vol.2
, Issue.7
, pp. 581-587
-
-
De Clercq, E.1
-
53
-
-
77955108676
-
Novel monocyclam derivatives as HIV entry inhibitors: Design synthesis, anti-HIV evaluation, and their interaction with the CXCR4 co-receptor
-
Pettersson S, Perez-Nueno VI, Mena MP, et al. Novel monocyclam derivatives as HIV entry inhibitors: Design, synthesis, anti-HIV evaluation, and their interaction with the CXCR4 co-receptor. ChemMedChem 2010;5:1272-81
-
(2010)
ChemMedChem
, vol.5
, pp. 1272-1281
-
-
Pettersson, S.1
Perez-Nueno, V.I.2
Mena, M.P.3
-
54
-
-
36148957078
-
Discover of small molecule CXCR4 Antagonists
-
Weiqiang Z, Zhongxing L, Aizhi Z, et al. Discover of small molecule CXCR4 Antagonists. J Med Chem 2007;50:5655-64
-
(2007)
J Med Chem
, vol.50
, pp. 5655-5664
-
-
Weiqiang, Z.1
Zhongxing, L.2
Aizhi, Z.3
-
55
-
-
78650336969
-
Dipyridine amines: A novel class of chemokine receptor type 4 antagonists with high specificity
-
Zhu A, Zhan W, Liang Z, et al. Dipyridine amines: A novel class of chemokine receptor type 4 antagonists with high specificity. J Med Chem 2010;53:8556-68
-
(2010)
J Med Chem
, vol.53
, pp. 8556-8568
-
-
Zhu, A.1
Zhan, W.2
Liang, Z.3
-
56
-
-
77249163222
-
Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: Analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication
-
Bridger GJ, Skerlj RT, Hernandez-Abad PE, et al. Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: Analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication. J Med Chem 2010;53:1250-60
-
(2010)
J Med Chem
, vol.53
, pp. 1250-1260
-
-
Bridger, G.J.1
Skerlj, R.T.2
Hernandez-Abad, P.E.3
-
57
-
-
77951100819
-
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication
-
Skerlj RT, Bridger GJ, Kaller A, et al. Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem 2010;53:3376-88
-
(2010)
J Med Chem
, vol.53
, pp. 3376-3388
-
-
Skerlj, R.T.1
Bridger, G.J.2
Kaller, A.3
-
58
-
-
0036846898
-
New anti-HIV agents and targets
-
DOI 10.1002/med.10021
-
De Clercq E. New anti-HIV agents and targets. Med Res Rev 2002;22:531-65 (Pubitemid 35299533)
-
(2002)
Medicinal Research Reviews
, vol.22
, Issue.6
, pp. 531-565
-
-
De Clercq, E.1
-
59
-
-
34447286192
-
Multiple-dose escalation study of the safety, pharmacokinetics, and biologic activity of oral AMD070, a selective CXCR4 receptor inhibitor, in human subjects
-
DOI 10.1128/AAC.00013-07
-
Stone ND, Dunaway SB, Flexner C, et al. Multiple-dose escalation study of the safety, pharmacokinetics, and biologic activity of oral AMD070, a selective CXCR4 receptor inhibitor, in human subjects. Antimicrob Agents Chemother 2007;51:2351-8 (Pubitemid 47047310)
-
(2007)
Antimicrobial Agents and Chemotherapy
, vol.51
, Issue.7
, pp. 2351-2358
-
-
Stone, N.D.1
Dunaway, S.B.2
Flexner, C.3
Tierney, C.4
Calandra, G.B.5
Becker, S.6
Cao, Y.-J.7
Wiggins, I.P.8
Conley, J.9
MacFarland, R.T.10
Park, J.-G.11
Lalama, C.12
Snyder, S.13
Kallungal, B.14
Klingman, K.L.15
Hendrix, C.W.16
-
60
-
-
68349150601
-
Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8- quinolinamines as CXCR4 antagonists with potent activity against HIV-1
-
Gudmundsson KS, Sebahar PR, Richardson LD, et al. Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1. Bioorg Med Chem Lett 2009;19:5048-52
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 5048-5052
-
-
Gudmundsson, K.S.1
Sebahar, P.R.2
Richardson, L.D.3
-
61
-
-
77949490788
-
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents
-
Miller JF, Turner EM, Gudmundsson KS, et al. Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents. Bioorg Med Chem Lett 2010;20:2125-8
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 2125-2128
-
-
Miller, J.F.1
Turner, E.M.2
Gudmundsson, K.S.3
-
62
-
-
77949487129
-
Synthesis of a novel tricyclic 1,2,3,4,4a,5,6,10b-octahydro-1,10- phenanthroline ring system and CXCR4 antagonists with potent activity against HIV-1
-
Catalano JG, Gudmundsson KS, Svolto A, et al. Synthesis of a novel tricyclic 1,2,3,4,4a,5,6,10b-octahydro-1,10-phenanthroline ring system and CXCR4 antagonists with potent activity against HIV-1. Bioorg Med Chem Lett 2010;20:2186-90
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 2186-2190
-
-
Catalano, J.G.1
Gudmundsson, K.S.2
Svolto, A.3
-
63
-
-
47149090722
-
Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach
-
Ueda S, Kato M, Inuki S, et al. Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach. Bioorg Med Chem Lett 2008;18:4124-9
-
(2008)
Bioorg Med Chem Lett
, vol.18
, pp. 4124-4129
-
-
Ueda, S.1
Kato, M.2
Inuki, S.3
-
64
-
-
33744830581
-
Identification of a new class of low molecular weight antagonists against the chemokine receptor CXCR4 having the dipicolylamine-zinc(II) complex structure
-
DOI 10.1021/jm060025u
-
Tamamura H, Ojida A, Ogawa T, et al. Identification of a new class of low molecular weight antagonists against the chemokine receptor CXCR4 having the dipicolylamine-zinc(II) complex structure. J Med Chem 2006;49:3412-15 (Pubitemid 43830540)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.11
, pp. 3412-3415
-
-
Tamamura, H.1
Ojida, A.2
Ogawa, T.3
Tsutsumi, H.4
Masuno, H.5
Nakashima, H.6
Yamamoto, N.7
Hamachi, I.8
Fujii, N.9
-
65
-
-
79955025109
-
Azamacrocyclic metal complexes as CXCR4 antagonists
-
Tanaka T, Narumi T, Ozaki T, et al. Azamacrocyclic metal complexes as CXCR4 antagonists. ChemMedChem 2011;6:834-9
-
(2011)
ChemMedChem
, vol.6
, pp. 834-839
-
-
Tanaka, T.1
Narumi, T.2
Ozaki, T.3
-
66
-
-
0037388121
-
A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity
-
DOI 10.1073/pnas.0630420100
-
Ichiyama K, Yokoyama-Kumakura S, Tanaka Y, et al. A duodenally absorbable CXC chemokine receptor 4 antagonist, KRH-1636, exhibits a potent and selective anti-HIV-1 activity. Proc Natl Acad Sci USA 2003;100:4185-90. The development of a non-peptidic CXCR4 antagonist KRH-1636. (Pubitemid 36418178)
-
(2003)
Proceedings of the National Academy of Sciences of the United States of America
, vol.100
, Issue.7
, 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
-
67
-
-
67449083566
-
Efficient inhibition of SDF-1alpha-mediated chemotaxis and HIV-1 infection by novel CXCR4 antagonists
-
Iwasaki Y, Akari H, Murakami T, et al. Efficient inhibition of SDF-1alpha-mediated chemotaxis and HIV-1 infection by novel CXCR4 antagonists. Cancer Sci 2009;100:778-81
-
(2009)
Cancer Sci
, vol.100
, pp. 778-781
-
-
Iwasaki, Y.1
Akari, H.2
Murakami, T.3
-
68
-
-
15444377047
-
Bioluminescence resonance energy transfer reveals ligand-induced conformational changes in CXCR4 homo- and heterodimers
-
DOI 10.1074/jbc.M411151200
-
Percherancier Y, Berchiche YA, Slight I, et al. Bioluminescence resonance energy transfer reveals ligand-induced conformational changes in CXCR4 homo-and heterodimers. J Biol Chem 2005;280:9895-903 (Pubitemid 40395837)
-
(2005)
Journal of Biological Chemistry
, vol.280
, Issue.11
, pp. 9895-9903
-
-
Percherancier, Y.1
Berchiche, Y.A.2
Slight, I.3
Volkmer-Engert, R.4
Tamamura, H.5
Fujii, N.6
Bouvier, M.7
Heveker, N.8
-
69
-
-
34247158219
-
i activation
-
DOI 10.1074/jbc.C600270200
-
Berchiche YA, Chow KY, Lagane B, et al. Direct assessment of CXCR4 mutant conformations reveals complex link between receptor structure and G(alpha)(i) activation. J Biol Chem 2007;282:5111-15 (Pubitemid 47093712)
-
(2007)
Journal of Biological Chemistry
, vol.282
, Issue.8
, pp. 5111-5115
-
-
Berchiche, Y.A.1
Chow, K.Y.2
Lagane, B.3
Leduc, M.4
Percherancier, Y.5
Fujii, N.6
Tamamura, H.7
Bachelerie, F.8
Heveker, N.9
-
70
-
-
78449262856
-
Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells
-
Tanaka T, Nomura W, Narumi T, et al. Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells. J Am Chem Soc 2010;132:15899-901
-
(2010)
J Am Chem Soc
, vol.132
, pp. 15899-15901
-
-
Tanaka, T.1
Nomura, W.2
Narumi, T.3
-
71
-
-
0031434606
-
Molecular mechanisms in retrovirus DNA integration
-
DOI 10.1016/S0166-3542(97)00046-6, PII S0166354297000466
-
Asante-Appiah E, Skalka AM. Molecular mechanisms in retrovirus DNA integration. Antiviral Res 1997;36:139-56 (Pubitemid 28031997)
-
(1997)
Antiviral Research
, vol.36
, Issue.3
, pp. 139-156
-
-
Asante-Appiah, E.1
Skalka, A.M.2
-
74
-
-
0028125329
-
Formation of a stable complex between the human immunodeficiency virus integrase protein and viral DNA
-
Vink C, Lutzke RAP, Plasterk RHA. Formation of a stable complex between the human immunodeficiency virus integrase protein and viral DNA. Nucleic Acids Res 1994;22:4103-10 (Pubitemid 24322711)
-
(1994)
Nucleic Acids Research
, vol.22
, Issue.20
, pp. 4103-4110
-
-
Vink, C.1
Puras Lutzke, R.A.2
Plasterk, R.H.A.3
-
75
-
-
0030051081
-
The role of manganese in promoting multimerization and assembly of human immunodeficiency virus type 1 integrase as a catalytically active complex on immobilized long terminal repeat substrates
-
Wolfe AL, Felock PJ, Hastings JC, et al. The role of manganese in promoting multimerization and assembly of human immunodeficiency virus type 1 integrase as a catalytically active complex on immobilized long terminal repeat substrates. J Virol 1996;70:1424-32 (Pubitemid 26062899)
-
(1996)
Journal of Virology
, vol.70
, Issue.3
, pp. 1424-1432
-
-
Wolfe, A.L.1
Felock, P.J.2
Hastings, J.C.3
Blau, C.U.4
Hazuda, D.J.5
-
76
-
-
0037076324
-
Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes
-
DOI 10.1073/pnas.092056199
-
Grobler JA, Stillmock K, Hu B, et al. Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci USA 2002;99:6661-6 (Pubitemid 34526189)
-
(2002)
Proceedings of the National Academy of Sciences of the United States of America
, vol.99
, Issue.10
, 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
-
77
-
-
3242769788
-
Integrase inhibitors and cellular immunity suppress retrovir replication in rhesus macaques
-
DOI 10.1126/science.1098632
-
Hazuda DJ, Young SD, Guare JP, et al. Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science 2004;305:528-32 (Pubitemid 38971345)
-
(2004)
Science
, vol.305
, Issue.5683
, pp. 528-532
-
-
Hazuda, D.J.1
Young, S.D.2
Guare, J.P.3
Anthony, N.J.4
Gomez, R.P.5
Wai, J.S.6
Vacca, J.P.7
Handt, L.8
Motzel, S.L.9
Klein, H.J.10
Dornadula, G.11
Danovich, R.M.12
Witmer, M.V.13
Wilson, K.A.A.14
Tussey, L.15
Schleif, W.A.16
Gabryelski, L.S.17
Jin, L.18
Miller, M.D.19
Casimiro, D.R.20
Emini, E.A.21
Shiver, J.W.22
more..
-
79
-
-
36749048641
-
Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects
-
DOI 10.1128/AAC.00716-07
-
Reddy YS, Min SS, Borland J, et al. Safety and pharmacokinetics of GSK364735, a human immunodeficiency virus type 1 integrase inhibitor, following single and repeated administration in healthy adult subjects. Antimicrob Agents Chemother 2007;51:4284-9 (Pubitemid 350209878)
-
(2007)
Antimicrobial Agents and Chemotherapy
, vol.51
, Issue.12
, pp. 4284-4289
-
-
Reddy, Y.S.1
Min, S.S.2
Borland, J.3
Song, I.4
Lin, J.5
Palleja, S.6
Symonds, W.T.7
-
80
-
-
62949153971
-
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase
-
Jones GS, Yu F, Zeynalzadegan A, et al. Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. Antimicrob Agents Chemother 2009;53:1194-203
-
(2009)
Antimicrob Agents Chemother
, vol.53
, pp. 1194-1203
-
-
Jones, G.S.1
Yu, F.2
Zeynalzadegan, A.3
-
81
-
-
35348957299
-
Synthesis of a hexahydropyrimido[1,2-a]azepine-2-carboxamide derivative useful as an HIV integrase inhibitor
-
DOI 10.1016/j.tetlet.2007.09.072, PII S0040403907018515
-
Ferrara M, Crescenzi B, Donghi M, et al. Synthesis of a hexahydropyrimido[1,2-a]azepine-2-carboxamide derivative useful as an HIV integrase inhibitor. Tetrahedron Lett 2007;48:8379-82 (Pubitemid 47615082)
-
(2007)
Tetrahedron Letters
, vol.48
, Issue.47
, pp. 8379-8382
-
-
Ferrara, M.1
Crescenzi, B.2
Donghi, M.3
Muraglia, E.4
Nizi, E.5
Pesci, S.6
Summa, V.7
Gardelli, C.8
-
82
-
-
33644863638
-
Novel HIV-1 integrase inhibitors derived from quinolone antibiotics
-
DOI 10.1021/jm0600139
-
Sato M, Motomura T, Aramaki H, et al. Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. J Med Chem 2006;49:1506-8. The development of an integrase inhibitor Elvitegravir. (Pubitemid 43376497)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.5
, pp. 1506-1508
-
-
Sato, M.1
Motomura, T.2
Aramaki, H.3
Matsuda, T.4
Yamashita, M.5
Ito, Y.6
Kawakami, H.7
Matsuzaki, Y.8
Watanabe, W.9
Yamataka, K.10
Ikeda, S.11
Kodama, E.12
Matsuoka, M.13
Shinkai, H.14
-
83
-
-
33748113778
-
Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients
-
DOI 10.1097/01.qai.0000233308.82860.2f, PII 0012633420060900000001
-
DeJesus E, Berger D, Markowitz M, et al. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. J Acquir Immune Defic Syndr 2006;43:1-5 (Pubitemid 44306480)
-
(2006)
Journal of Acquired Immune Deficiency Syndromes
, vol.43
, Issue.1
, pp. 1-5
-
-
DeJesus, E.1
Berger, D.2
Markowitz, M.3
Cohen, C.4
Hawkins, T.5
Ruane, P.6
Elion, R.7
Farthing, C.8
Zhong, L.9
Cheng, A.K.10
McColl, D.11
Kearney, B.P.12
-
84
-
-
77149123315
-
Pharmacokinetics and pharmacodynamics of GS-9350: A novel pharmacokinetic enhancer without anti-HIV activity
-
Mathias AA, German P, Murray BP, et al. Pharmacokinetics and pharmacodynamics of GS-9350: A novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther 2010;87:322-9
-
(2010)
Clin Pharmacol Ther
, vol.87
, pp. 322-329
-
-
Mathias, A.A.1
German, P.2
Murray, B.P.3
-
85
-
-
51549116289
-
Comparison of Raltegravir and Elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants
-
Marinello J, Marchand C, Mott BT, et al. Comparison of Raltegravir and Elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. Biochemistry 2008;47:9345-54
-
(2008)
Biochemistry
, vol.47
, pp. 9345-9354
-
-
Marinello, J.1
Marchand, C.2
Mott, B.T.3
-
86
-
-
77956017859
-
Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor
-
The development of an integrase inhibitor MK-2048
-
Bar-Magen T, Sloan RD, Donahue DA, et al. Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor. J Virol 2010;84:9210-16. The development of an integrase inhibitor MK-2048.
-
(2010)
J Virol
, vol.84
, pp. 9210-9216
-
-
Bar-Magen, T.1
Sloan, R.D.2
Donahue, D.A.3
-
87
-
-
56849131000
-
Advances in two-metal chelation inhibitors of HIV integrase
-
Johns BA, Svolto AC. Advances in two-metal chelation inhibitors of HIV integrase. Expert Opin Ther Patents 2008;18:1225-37
-
(2008)
Expert Opin Ther Patents
, vol.18
, pp. 1225-1237
-
-
Johns, B.A.1
Svolto, A.C.2
-
88
-
-
73849124557
-
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. ?
-
The development of an integrase inhibitor Dolutegravir
-
Min S, Song I, Borland J, et al. Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. ?Antimicrob Agents Chemother 2010;54:254-8. The development of an integrase inhibitor Dolutegravir.
-
(2010)
Antimicrob Agents Chemother
, vol.54
, pp. 254-258
-
-
Min, S.1
Song, I.2
Borland, J.3
-
89
-
-
78751697293
-
Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor
-
Kobayashi M, Yoshinaga T, Seki T, et al. In vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother 2011;55:813-21
-
(2011)
Antimicrob Agents Chemother
, vol.55
, pp. 813-821
-
-
Kobayashi, M.1
Yoshinaga, T.2
Seki, T.3
-
90
-
-
9244252539
-
Globoidnan A: A lignan from Eucalyptus globoidea inhibits HIV integrase
-
DOI 10.1016/j.phytochem.2004.10.006, PII S0031942204005266
-
Ovenden SP, Yu J, Wan SS, et al. Globoidnan A: A lignan from Eucalyptus globoidea inhibits HIV integrase. Phytochemistry 2004;65:3255-9 (Pubitemid 39550393)
-
(2004)
Phytochemistry
, vol.65
, Issue.24
, pp. 3255-3259
-
-
Ovenden, S.P.B.1
Yu, J.2
San Wan, S.3
Sberna, G.4
Murray Tait, R.5
Rhodes, D.6
Cox, S.7
Coates, J.8
Walsh, N.G.9
Meurer-Grimes, B.M.10
-
91
-
-
58549092798
-
Functional and structural characterization of the integrase from the prototype foamy virus
-
Valkov E, Gupta SS, Hare S, et al. Functional and structural characterization of the integrase from the prototype foamy virus. Nucleic Acids Res 2009;37:243-55
-
(2009)
Nucleic Acids Res
, vol.37
, pp. 243-255
-
-
Valkov, E.1
Gupta, S.S.2
Hare, S.3
-
92
-
-
77949365510
-
Retroviral intasome assembly and inhibition of DNA strand transfer
-
Hare S, Gupta SS, Valkov E, et al. Retroviral intasome assembly and inhibition of DNA strand transfer. Nature 2010;464:232-6
-
(2010)
Nature
, vol.464
, pp. 232-236
-
-
Hare, S.1
Gupta, S.S.2
Valkov, E.3
-
93
-
-
79151481013
-
HIV-1 integrase strand-transfer inhibitors: Design, synthesis and molecular modeling investigation
-
De Luca L, De Grazia S, Ferro S, et al. HIV-1 integrase strand-transfer inhibitors: Design, synthesis and molecular modeling investigation. Eur J Med Chem 2011;46:756-64
-
(2011)
Eur J Med Chem
, vol.46
, pp. 756-764
-
-
De Luca, L.1
De Grazia, S.2
Ferro, S.3
-
94
-
-
77954748209
-
Peptide HIV-1 integrase inhibitors from HIV-1 gene products
-
Suzuki S, Urano E, Hashimoto C, et al. Peptide HIV-1 integrase inhibitors from HIV-1 gene products. J Med Chem 2010;53:5356-60
-
(2010)
J Med Chem
, vol.53
, pp. 5356-5360
-
-
Suzuki, S.1
Urano, E.2
Hashimoto, C.3
-
95
-
-
77956339915
-
Peptidic HIV integrase inhibitors derived from HIV gene products: Structure-activity relationship studies
-
Suzuki S, Maddali K, Hashimoto C, et al. Peptidic HIV integrase inhibitors derived from HIV gene products: Structure-activity relationship studies. Bioorg Med Chem 2010;18:6771-5
-
(2010)
Bioorg Med Chem
, vol.18
, pp. 6771-6775
-
-
Suzuki, S.1
Maddali, K.2
Hashimoto, C.3
-
96
-
-
23844440296
-
Identification of N-phenyl-N′-(2,2,6,6-tetramethyl-piperidin-4-yl)- oxalamides as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4
-
DOI 10.1016/j.virol.2005.06.008, PII S0042682205003363
-
Zhao Q, Ma L, Jiang S, et al. Identification of N-phenyl-N'-(2,2,6,6- tetramethyl-piperidin-4-yl)-oxalamides as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4. Virology 2005;339:213-25 (Pubitemid 41169789)
-
(2005)
Virology
, vol.339
, Issue.2
, pp. 213-225
-
-
Zhao, Q.1
Ma, L.2
Jiang, S.3
Lu, H.4
Liu, S.5
He, Y.6
Strick, N.7
Neamati, N.8
Debnath, A.K.9
-
97
-
-
33748491260
-
Thermodynamics of binding of a low-molecular-weight CD4 mimetic to HIV-1 gp120
-
DOI 10.1021/bi061193r
-
Schon A, Madani N, Klein JC, et al. Thermodynamics of binding of a low-molecular-weight CD4 mimetic to HIV-1 gp120. Biochemistry 2006;45:10973-80 (Pubitemid 44360167)
-
(2006)
Biochemistry
, vol.45
, Issue.36
, pp. 10973-10980
-
-
Schon, A.1
Madani, N.2
Klein, J.C.3
Hubicki, A.4
Ng, D.5
Yang, X.6
Smith III, A.B.7
Sodroski, J.8
Freire, E.9
-
99
-
-
77957591864
-
CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist
-
Narumi T, Ochiai C, Yoshimura K, et al. CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. Bioorg Med Chem Lett 2010;20:5853-8
-
(2010)
Bioorg Med Chem Lett
, vol.20
, pp. 5853-5958
-
-
Narumi, T.1
Ochiai, C.2
Yoshimura, K.3
-
100
-
-
77954525340
-
Enhanced exposure of human immunodeficiency virus type 1 primary isolate neutralization epitopes through binding of CD4 mimetic compounds
-
Yoshimura K, Harada S, Shibata J, et al. Enhanced exposure of human immunodeficiency virus type 1 primary isolate neutralization epitopes through binding of CD4 mimetic compounds. J Virol 2010;84:7558-68
-
(2010)
J Virol
, vol.84
, pp. 7558-7568
-
-
Yoshimura, K.1
Harada, S.2
Shibata, J.3
-
101
-
-
78650721466
-
Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening
-
Lalonde JM, Elban MA, Courter JR, et al. Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening. Bioorg Med Chem 2011;19:91-101
-
(2011)
Bioorg Med Chem
, vol.19
, pp. 91-101
-
-
Lalonde, J.M.1
Elban, M.A.2
Courter, J.R.3
-
102
-
-
37349002730
-
Design and synthesis of human immunodeficiency virus entry inhibitors: Sulfonamide as an isostere for the α-ketoamide group
-
DOI 10.1021/jm070650e
-
Lu RJ, Tucker JA, Zinevitch T, et al. Design and synthesis of human immunodeficiency virus entryinhibitors: Sulfonamide as an isostere for the alpha-ketoamide group. J Med Chem 2007;50:6535-44 (Pubitemid 350309093)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.26
, pp. 6535-6544
-
-
Lu, R.-J.1
Tucker, J.A.2
Zinevitch, T.3
Kirichenko, O.4
Konoplev, V.5
Kuznetsova, S.6
Sviridov, S.7
Pickens, J.8
Tandel, S.9
Brahmachary, E.10
Yang, Y.11
Wang, J.12
Freel, S.13
Fisher, S.14
Sullivan, A.15
Zhou, J.16
Stanfield-Oakley, S.17
Greenberg, M.18
Bolognesi, D.19
Bray, B.20
Koszalka, B.21
Jeffs, P.22
Khasanov, A.23
Ma, Y.-A.24
Jeffries, C.25
Liu, C.26
Proskurina, T.27
Zhu, T.28
Chucholowski, A.29
Li, R.30
Sexton, C.31
more..
-
103
-
-
0032507962
-
Function of the chemokine receptor CXCR4 in heaematopolesis and in cerebellar development
-
DOI 10.1038/31269
-
Zou Y-R, Kottmann AH, Kuroda M, et al. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature 1998;393:595-9 (Pubitemid 28319251)
-
(1998)
Nature
, vol.393
, Issue.6685
, pp. 595-599
-
-
Zou, Y.-R.1
Kottman, A.H.2
Kuroda, M.3
Taniuchi, I.4
Littman, D.R.5
-
104
-
-
44449125062
-
Potent synergistic anti-Human Immunodeficiency Virus (HIV) effects using combinations of the CCR5 inhibitor aplaviroc with other anti-HIV drugs
-
DOI 10.1128/AAC.01299-07
-
Nakata H, Steinberg SM, Koh Y, et al. Potent synergistic anti-human immunodeficiency virus (HIV) effects using combinations of the CCR5 inhibitor aplaviroc with other anti-HIV drugs. Antimicrob Agents Chemother 2008;52:2111-19 (Pubitemid 351758548)
-
(2008)
Antimicrobial Agents and Chemotherapy
, vol.52
, Issue.6
, pp. 2111-2119
-
-
Nakata, H.1
Steinberg, S.M.2
Kon, Y.3
Maeda, K.4
Takaoka, Y.5
Tamamura, H.6
Fujii, N.7
Mitsuya, H.8
-
105
-
-
34748870155
-
Enhanced unique pattern of hematopoietic cell mobilization induced by the CXCR4 antagonist4F-benzoyl-TN14003
-
Abraham M, Biyder K, Begin M, et al. Enhanced unique pattern of hematopoietic cell mobilization induced by the CXCR4 antagonist4F-benzoyl- TN14003. Stem Cells 2007; 25:2158-6.
-
(2007)
Stem Cells
, vol.25
, pp. 2158-2186
-
-
Abraham, M.1
Biyder, K.2
Begin, M.3
-
106
-
-
20944440068
-
Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist
-
DOI 10.1084/jem.20041385
-
Broxmeyer HE, Orschell CM, Clapp DW, et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med 2005;201:1307-18 (Pubitemid 40629073)
-
(2005)
Journal of Experimental Medicine
, vol.201
, Issue.8
, pp. 1307-1318
-
-
Broxmeyer, H.E.1
Orschell, C.M.2
Clapp, D.W.3
Hangoc, G.4
Cooper, S.5
Plett, P.A.6
Liles, W.C.7
Li, X.8
Graham-Evans, B.9
Campbell, T.B.10
Calandra, G.11
Bridger, G.12
Dale, D.C.13
Srour, E.F.14
-
107
-
-
0141923918
-
Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist
-
DOI 10.1182/blood-2003-02-0663
-
Liles WC, Broxmeyer HE, Rodger E, et al. Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist. Blood 2003;102:2728-30 (Pubitemid 37248839)
-
(2003)
Blood
, vol.102
, Issue.8
, pp. 2728-2730
-
-
Liles, W.C.1
Broxmeyer, H.E.2
Rodger, E.3
Wood, B.4
Hubel, K.5
Cooper, S.6
Hangoc, G.7
Bridger, G.J.8
Henson, G.W.9
Calandra, G.10
Dale, D.C.11
-
108
-
-
10744226241
-
Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro
-
DOI 10.1128/AAC.47.10.3123-3129.2003
-
Koh Y, Nakata H, Maeda K, et al. Novel bis-tetrahydrofuranylurethane- containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother 2003;47:3123-9 (Pubitemid 37229567)
-
(2003)
Antimicrobial Agents and Chemotherapy
, vol.47
, Issue.10
, pp. 3123-3129
-
-
Koh, Y.1
Nakata, H.2
Maeda, K.3
Ogata, H.4
Bilcer, G.5
Devasamudram, T.6
Kincaid, J.F.7
Boross, P.8
Wang, Y.-F.9
Tie, Y.10
Volarath, P.11
Gaddis, L.12
Harrison, R.W.13
Weber, I.T.14
Ghosh, A.K.15
Mitsuya, H.16
-
109
-
-
33747479539
-
Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance
-
DOI 10.1021/jm060561m
-
Ghosh AK, Sridhar PR, Leshchenko S, et al. Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance. J Med Chem 2006;49:5252-61 (Pubitemid 44260221)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.17
, pp. 5252-5261
-
-
Ghosh, A.K.1
Sridhar, P.R.2
Leshchenko, S.3
Hussain, A.K.4
Li, J.5
Kovalevsky, A.Yu.6
Walters, D.E.7
Wedekind, J.E.8
Grum-Tokars, V.9
Das, D.10
Koh, Y.11
Maeda, K.12
Gatanaga, H.13
Weber, I.T.14
Mitsuya, H.15
|