-
1
-
-
52449097240
-
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection
-
Summa, V., Petrocchi, A., Bonelli, F., Crescenzi, B., Donghi, M., Ferrara, M., Fiore, F., Gardelli, C., Gonzalez Paz, O., Hazuda, D. J., Jones, P., Kinzel, O., Laufer, R., Monteagudo, E., Muraglia, E., Nizi, E., Orvieto, F., Pace, P., Pescatore, G., Scarpelli, R., Stillmock, K., Witmer, M. V., and Rowley, M. (2008) Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection J. Med. Chem. 51, 5843-5855
-
(2008)
J. Med. Chem.
, vol.51
, pp. 5843-5855
-
-
Summa, V.1
Petrocchi, A.2
Bonelli, F.3
Crescenzi, B.4
Donghi, M.5
Ferrara, M.6
Fiore, F.7
Gardelli, C.8
Gonzalez Paz, O.9
Hazuda, D.J.10
Jones, P.11
Kinzel, O.12
Laufer, R.13
Monteagudo, E.14
Muraglia, E.15
Nizi, E.16
Orvieto, F.17
Pace, P.18
Pescatore, G.19
Scarpelli, R.20
Stillmock, K.21
Witmer, M.V.22
Rowley, M.23
more..
-
2
-
-
33845366857
-
Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals
-
Markowitz, M., Morales-Ramirez, J. O., Nguyen, B. Y., Kovacs, C. M., Steigbigel, R. T., Cooper, D. A., Liporace, R., Schwartz, R., Isaacs, R., Gilde, L. R., Wenning, L., Zhao, J., and Teppler, H. (2006) Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals J. Acquired Immune Defic. Syndr. 43, 509-515
-
(2006)
J. Acquired Immune Defic. Syndr.
, vol.43
, pp. 509-515
-
-
Markowitz, M.1
Morales-Ramirez, J.O.2
Nguyen, B.Y.3
Kovacs, C.M.4
Steigbigel, R.T.5
Cooper, D.A.6
Liporace, R.7
Schwartz, R.8
Isaacs, R.9
Gilde, L.R.10
Wenning, L.11
Zhao, J.12
Teppler, H.13
-
3
-
-
47949120697
-
Raltegravir with optimized background therapy for resistant HIV-1 infection
-
Steigbigel, R. T., Cooper, D. A., Kumar, P. N., Eron, J. E., Schechter, M., Markowitz, M., Loutfy, M. R., Lennox, J. L., Gatell, J. M., Rockstroh, J. K., Katlama, C., Yeni, P., Lazzarin, A., Clotet, B., Zhao, J., Chen, J., Ryan, D. M., Rhodes, R. R., Killar, J. A., Gilde, L. R., Strohmaier, K. M., Meibohm, A. R., Miller, M. D., Hazuda, D. J., Nessly, M. L., DiNubile, M. J., Isaacs, R. D., Nguyen, B. Y., and Teppler, H. (2008) Raltegravir with optimized background therapy for resistant HIV-1 infection N. Engl. J. Med. 359, 339-354
-
(2008)
N. Engl. J. Med.
, vol.359
, pp. 339-354
-
-
Steigbigel, R.T.1
Cooper, D.A.2
Kumar, P.N.3
Eron, J.E.4
Schechter, M.5
Markowitz, M.6
Loutfy, M.R.7
Lennox, J.L.8
Gatell, J.M.9
Rockstroh, J.K.10
Katlama, C.11
Yeni, P.12
Lazzarin, A.13
Clotet, B.14
Zhao, J.15
Chen, J.16
Ryan, D.M.17
Rhodes, R.R.18
Killar, J.A.19
Gilde, L.R.20
Strohmaier, K.M.21
Meibohm, A.R.22
Miller, M.D.23
Hazuda, D.J.24
Nessly, M.L.25
Dinubile, M.J.26
Isaacs, R.D.27
Nguyen, B.Y.28
Teppler, H.29
more..
-
4
-
-
69449101785
-
Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: A multicentre, double-blind randomised controlled trial
-
Lennox, J. L., DeJesus, E., Lazzarin, A., Pollard, R. B., Madruga, J. V., Berger, D. S., Zhao, J., Xu, X., Williams-Diaz, A., Rodgers, A. J., Barnard, R. J., Miller, M. D., DiNubile, M. J., Nguyen, B. Y., Leavitt, R., and Sklar, P. (2009) Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial Lancet 374, 796-806
-
(2009)
Lancet
, vol.374
, pp. 796-806
-
-
Lennox, J.L.1
Dejesus, E.2
Lazzarin, A.3
Pollard, R.B.4
Madruga, J.V.5
Berger, D.S.6
Zhao, J.7
Xu, X.8
Williams-Diaz, A.9
Rodgers, A.J.10
Barnard, R.J.11
Miller, M.D.12
Dinubile, M.J.13
Nguyen, B.Y.14
Leavitt, R.15
Sklar, P.16
-
5
-
-
65549085822
-
Characterization and structural analysis of HIV-1 integrase conservation
-
Ceccherini-Silberstein, F., Malet, I., D'Arrigo, R., Antinori, A., Marcelin, A. G., and Perno, C. F. (2009) Characterization and structural analysis of HIV-1 integrase conservation AIDS Rev. 11, 17-29
-
(2009)
AIDS Rev.
, vol.11
, pp. 17-29
-
-
Ceccherini-Silberstein, F.1
Malet, I.2
D'Arrigo, R.3
Antinori, A.4
Marcelin, A.G.5
Perno, C.F.6
-
6
-
-
47949114939
-
Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection
-
Cooper, D. A., Steigbigel, R. T., Gatell, J. M., Rockstroh, J. K., Katlama, C., Yeni, P., Lazzarin, A., Clotet, B., Kumar, P. N., Eron, J. E., Schechter, M., Markowitz, M., Loutfy, M. R., Lennox, J. L., Zhao, J., Chen, J., Ryan, D. M., Rhodes, R. R., Killar, J. A., Gilde, L. R., Strohmaier, K. M., Meibohm, A. R., Miller, M. D., Hazuda, D. J., Nessly, M. L., DiNubile, M. J., Isaacs, R. D., Teppler, H., and Nguyen, B. Y. (2008) Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection N. Engl. J. Med. 359, 355-365
-
(2008)
N. Engl. J. Med.
, vol.359
, pp. 355-365
-
-
Cooper, D.A.1
Steigbigel, R.T.2
Gatell, J.M.3
Rockstroh, J.K.4
Katlama, C.5
Yeni, P.6
Lazzarin, A.7
Clotet, B.8
Kumar, P.N.9
Eron, J.E.10
Schechter, M.11
Markowitz, M.12
Loutfy, M.R.13
Lennox, J.L.14
Zhao, J.15
Chen, J.16
Ryan, D.M.17
Rhodes, R.R.18
Killar, J.A.19
Gilde, L.R.20
Strohmaier, K.M.21
Meibohm, A.R.22
Miller, M.D.23
Hazuda, D.J.24
Nessly, M.L.25
Dinubile, M.J.26
Isaacs, R.D.27
Teppler, H.28
Nguyen, B.Y.29
more..
-
7
-
-
70350666377
-
Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred by multiple non-overlapping genetic pathways
-
Fransen, S., Gupta, S., Danovich, R., Hazuda, D., Miller, M., Witmer, M., Petropoulos, C. J., and Huang, W. (2009) Loss of raltegravir susceptibility by human immunodeficiency virus type 1 is conferred by multiple non-overlapping genetic pathways J. Virol. 83, 11440-11446
-
(2009)
J. Virol.
, vol.83
, pp. 11440-11446
-
-
Fransen, S.1
Gupta, S.2
Danovich, R.3
Hazuda, D.4
Miller, M.5
Witmer, M.6
Petropoulos, C.J.7
Huang, W.8
-
8
-
-
70349337790
-
Longitudinal analysis of raltegravir susceptibility and integrase replication capacity of human immunodeficiency virus type 1 during virologic failure
-
Fransen, S., Karmochkine, M., Huang, W., Weiss, L., Petropoulos, C. J., and Charpentier, C. (2009) Longitudinal analysis of raltegravir susceptibility and integrase replication capacity of human immunodeficiency virus type 1 during virologic failure Antimicrob. Agents Chemother. 53, 4522-4524
-
(2009)
Antimicrob. Agents Chemother.
, vol.53
, pp. 4522-4524
-
-
Fransen, S.1
Karmochkine, M.2
Huang, W.3
Weiss, L.4
Petropoulos, C.J.5
Charpentier, C.6
-
9
-
-
55249105017
-
Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitors
-
Goethals, O., Clayton, R., Van Ginderen, M., Vereycken, I., Wagemans, E., Geluykens, P., Dockx, K., Strijbos, R., Smits, V., Vos, A., Meersseman, G., Jochmans, D., Vermeire, K., Schols, D., Hallenberger, S., and Hertogs, K. (2008) Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitors J. Virol. 82, 10366-10374
-
(2008)
J. Virol.
, vol.82
, pp. 10366-10374
-
-
Goethals, O.1
Clayton, R.2
Van Ginderen, M.3
Vereycken, I.4
Wagemans, E.5
Geluykens, P.6
Dockx, K.7
Strijbos, R.8
Smits, V.9
Vos, A.10
Meersseman, G.11
Jochmans, D.12
Vermeire, K.13
Schols, D.14
Hallenberger, S.15
Hertogs, K.16
-
10
-
-
40549115791
-
-
in XVI International Drug Resistance Workshop, p, Barbados, West Indies.
-
McColl, D. J., Fransen, S., Gupta, S., Parkin, N., Margot, N., Chuck, S., Cheng, A. K., and Miller, M. D. (2007) Resistance and cross-resistance to first generation integrase inhibitors: insights from a Phase II study of elvitegravir (GS 9137), in XVI International Drug Resistance Workshop, p S11, Barbados, West Indies.
-
(2007)
Resistance and Cross-resistance to First Generation Integrase Inhibitors: Insights from A Phase II Study of Elvitegravir (GS 9137)
, pp. 11
-
-
McColl, D.J.1
Fransen, S.2
Gupta, S.3
Parkin, N.4
Margot, N.5
Chuck, S.6
Cheng, A.K.7
Miller, M.D.8
-
11
-
-
37849002059
-
Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)
-
Shimura, K., Kodama, E., Sakagami, Y., Matsuzaki, Y., Watanabe, W., Yamataka, K., Watanabe, Y., Ohata, Y., Doi, S., Sato, M., Kano, M., Ikeda, S., and Matsuoka, M. (2008) Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137) J. Virol. 82, 764-774
-
(2008)
J. Virol.
, vol.82
, pp. 764-774
-
-
Shimura, K.1
Kodama, E.2
Sakagami, Y.3
Matsuzaki, Y.4
Watanabe, W.5
Yamataka, K.6
Watanabe, Y.7
Ohata, Y.8
Doi, S.9
Sato, M.10
Kano, M.11
Ikeda, S.12
Matsuoka, M.13
-
12
-
-
73949084442
-
Raltegravir has no residual antiviral activity in vivo against HIV-1 with resistance-associated mutations to this drug
-
Wirden, M., Simon, A., Schneider, L., Tubiana, R., Malet, I., Ait-Mohand, H., Peytavin, G., Katlama, C., Calvez, V., and Marcelin, A. G. (2009) Raltegravir has no residual antiviral activity in vivo against HIV-1 with resistance-associated mutations to this drug J. Antimicrob. Chemother. 64, 1087-1090
-
(2009)
J. Antimicrob. Chemother.
, vol.64
, pp. 1087-1090
-
-
Wirden, M.1
Simon, A.2
Schneider, L.3
Tubiana, R.4
Malet, I.5
Ait-Mohand, H.6
Peytavin, G.7
Katlama, C.8
Calvez, V.9
Marcelin, A.G.10
-
13
-
-
36049049062
-
Inhibition of human immunodeficiency virus type 1 concerted integration by strand transfer inhibitors which recognize a transient structural intermediate
-
Pandey, K. K., Bera, S., Zahm, J., Vora, A., Stillmock, K., Hazuda, D., and Grandgenett, D. P. (2007) Inhibition of human immunodeficiency virus type 1 concerted integration by strand transfer inhibitors which recognize a transient structural intermediate J. Virol. 81, 12189-12199
-
(2007)
J. Virol.
, vol.81
, pp. 12189-12199
-
-
Pandey, K.K.1
Bera, S.2
Zahm, J.3
Vora, A.4
Stillmock, K.5
Hazuda, D.6
Grandgenett, D.P.7
-
14
-
-
33645285267
-
Retroviral DNA integration: Reaction pathway and critical intermediates
-
Li, M., Mizuuchi, M., Burke, T. R., Jr., and Craigie, R. (2006) Retroviral DNA integration: reaction pathway and critical intermediates EMBO J. 25, 1295-1304
-
(2006)
EMBO J.
, vol.25
, pp. 1295-1304
-
-
Li, M.1
Mizuuchi, M.2
Burke Jr., T.R.3
Craigie, R.4
-
15
-
-
67349245812
-
Molecular interactions between HIV-1 integrase and the two viral DNA ends within the synaptic complex that mediates concerted integration
-
Bera, S., Pandey, K. K., Vora, A. C., and Grandgenett, D. P. (2009) Molecular interactions between HIV-1 integrase and the two viral DNA ends within the synaptic complex that mediates concerted integration J. Mol. Biol. 389, 183-198
-
(2009)
J. Mol. Biol.
, vol.389
, pp. 183-198
-
-
Bera, S.1
Pandey, K.K.2
Vora, A.C.3
Grandgenett, D.P.4
-
16
-
-
77957040861
-
HIV-1 integrase strand transfer inhibitors: Novel insights into their mechanism of action
-
Pandey, K. K. and Grandgenett, D. P. (2008) HIV-1 integrase strand transfer inhibitors: novel insights into their mechanism of action Retrovirol.: Res. Treatment 2, 11-16
-
(2008)
Retrovirol.: Res. Treatment
, vol.2
, pp. 11-16
-
-
Pandey, K.K.1
Grandgenett, D.P.2
-
17
-
-
34247128760
-
Transcriptional coactivator LEDGF/p75 modulates human immunodeficiency virus type 1 integrase-mediated concerted integration
-
Pandey, K. K., Sinha, S., and Grandgenett, D. P. (2007) Transcriptional coactivator LEDGF/p75 modulates human immunodeficiency virus type 1 integrase-mediated concerted integration J. Virol. 81, 3969-3979
-
(2007)
J. Virol.
, vol.81
, pp. 3969-3979
-
-
Pandey, K.K.1
Sinha, S.2
Grandgenett, D.P.3
-
18
-
-
64649098171
-
Nucleoprotein complex intermediates in HIV-1 integration
-
Li, M. and Craigie, R. (2009) Nucleoprotein complex intermediates in HIV-1 integration Methods 47, 237-242
-
(2009)
Methods
, vol.47
, pp. 237-242
-
-
Li, M.1
Craigie, R.2
-
19
-
-
14244264128
-
HIV-1 integrase crosslinked oligomers are active in vitro
-
Faure, A., Calmels, C., Desjobert, C., Castroviejo, M., Caumont-Sarcos, A., Tarrago-Litvak, L., Litvak, S., and Parissi, V. (2005) HIV-1 integrase crosslinked oligomers are active in vitro Nucleic Acids Res. 33, 977-986
-
(2005)
Nucleic Acids Res.
, vol.33
, pp. 977-986
-
-
Faure, A.1
Calmels, C.2
Desjobert, C.3
Castroviejo, M.4
Caumont-Sarcos, A.5
Tarrago-Litvak, L.6
Litvak, S.7
Parissi, V.8
-
20
-
-
77949365510
-
Retroviral intasome assembly and inhibition of DNA strand transfer
-
Hare, S., Gupta, S. S., Valkov, E., Engelman, A., and Cherepanov, P. (2010) Retroviral intasome assembly and inhibition of DNA strand transfer Nature 464, 232-236
-
(2010)
Nature
, vol.464
, pp. 232-236
-
-
Hare, S.1
Gupta, S.S.2
Valkov, E.3
Engelman, A.4
Cherepanov, P.5
-
21
-
-
3843108916
-
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase
-
Hazuda, D. J., Anthony, N. J., Gomez, R. P., Jolly, S. M., Wai, J. S., Zhuang, L., Fisher, T. E., Embrey, M., Guare, J. P., Jr., Egbertson, M. S., Vacca, J. P., Huff, J. R., Felock, P. J., Witmer, M. V., Stillmock, K. A., Danovich, R., Grobler, J., Miller, M. D., Espeseth, A. S., Jin, L., Chen, I. W., Lin, J. H., Kassahun, K., Ellis, J. D., Wong, B. K., Xu, W., Pearson, P. G., Schleif, W. A., Cortese, R., Emini, E., Summa, V., Holloway, M. K., and Young, S. D. (2004) A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase Proc. Natl. Acad. Sci. U.S.A. 101, 11233-11238
-
(2004)
Proc. Natl. Acad. Sci. U.S.A.
, vol.101
, pp. 11233-11238
-
-
Hazuda, D.J.1
Anthony, N.J.2
Gomez, R.P.3
Jolly, S.M.4
Wai, J.S.5
Zhuang, L.6
Fisher, T.E.7
Embrey, M.8
Guare Jr., J.P.9
Egbertson, M.S.10
Vacca, J.P.11
Huff, J.R.12
Felock, P.J.13
Witmer, M.V.14
Stillmock, K.A.15
Danovich, R.16
Grobler, J.17
Miller, M.D.18
Espeseth, A.S.19
Jin, L.20
Chen, I.W.21
Lin, J.H.22
Kassahun, K.23
Ellis, J.D.24
Wong, B.K.25
Xu, W.26
Pearson, P.G.27
Schleif, W.A.28
Cortese, R.29
Emini, E.30
Summa, V.31
Holloway, M.K.32
Young, S.D.33
more..
-
22
-
-
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., and Miller, M. D. (2000) Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells Science 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
-
23
-
-
64649083538
-
Selection and analysis of HIV-1 integrase strand transfer inhibitor resistant mutant viruses
-
Witmer, M. and Danovich, R. (2009) Selection and analysis of HIV-1 integrase strand transfer inhibitor resistant mutant viruses Methods 47, 277-282
-
(2009)
Methods
, vol.47
, pp. 277-282
-
-
Witmer, M.1
Danovich, R.2
-
24
-
-
62149093020
-
The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation
-
Delelis, O., Malet, I., Na, L., Tchertanov, L., Calvez, V., Marcelin, A. G., Subra, F., Deprez, E., and Mouscadet, J. F. (2009) The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation Nucleic Acids Res. 37, 1193-1201
-
(2009)
Nucleic Acids Res.
, vol.37
, pp. 1193-1201
-
-
Delelis, O.1
Malet, I.2
Na, L.3
Tchertanov, L.4
Calvez, V.5
Marcelin, A.G.6
Subra, F.7
Deprez, E.8
Mouscadet, J.F.9
-
25
-
-
0033562537
-
Activity of recombinant HIV-1 integrase on mini-HIV DNA
-
Cherepanov, P., Surratt, D., Toelen, J., Pluymers, W., Griffith, J., De Clercq, E., and Debyser, Z. (1999) Activity of recombinant HIV-1 integrase on mini-HIV DNA Nucleic Acids Res. 27, 2202-2210
-
(1999)
Nucleic Acids Res.
, vol.27
, pp. 2202-2210
-
-
Cherepanov, P.1
Surratt, D.2
Toelen, J.3
Pluymers, W.4
Griffith, J.5
De Clercq, E.6
Debyser, Z.7
-
26
-
-
0036118227
-
Efficient concerted integration by recombinant human immunodeficiency virus type 1 integrase without cellular or viral cofactors
-
Sinha, S., Pursley, M. H., and Grandgenett, D. P. (2002) Efficient concerted integration by recombinant human immunodeficiency virus type 1 integrase without cellular or viral cofactors J. Virol. 76, 3105-3113
-
(2002)
J. Virol.
, vol.76
, pp. 3105-3113
-
-
Sinha, S.1
Pursley, M.H.2
Grandgenett, D.P.3
-
27
-
-
64649089647
-
Biochemical and biophysical analyses of concerted (U5/U3) integration
-
Grandgenett, D. P., Bera, S., Pandey, K. K., Vora, A. C., Zahm, J., and Sinha, S. (2009) Biochemical and biophysical analyses of concerted (U5/U3) integration Methods 47, 229-236
-
(2009)
Methods
, vol.47
, pp. 229-236
-
-
Grandgenett, D.P.1
Bera, S.2
Pandey, K.K.3
Vora, A.C.4
Zahm, J.5
Sinha, S.6
-
28
-
-
77957033758
-
-
in 4 th International AIDS Society (IAS) Conference, July 22-25, 2007, Sydney, Australia.
-
Vacca, J., Wai, J., Fisher, T., Embrey, M., Hazuda, D., Miller, M., Felock, P., Witmer, M., Gabryelski, L., and Lyle, T. (2007) Discovery of MK-2048 - subtle changes confer unique resistance properties to a series of tricyclic hydroxypyrrole integrase strand transfer inhibitors, in 4 th International AIDS Society (IAS) Conference, July 22-25, 2007, Sydney, Australia.
-
(2007)
Discovery of MK-2048 - Subtle Changes Confer Unique Resistance Properties to A Series of Tricyclic Hydroxypyrrole Integrase Strand Transfer Inhibitors
-
-
Vacca, J.1
Wai, J.2
Fisher, T.3
Embrey, M.4
Hazuda, D.5
Miller, M.6
Felock, P.7
Witmer, M.8
Gabryelski, L.9
Lyle, T.10
-
29
-
-
77957061409
-
-
in 14 th Conference on Retroviruses and Opportunistic Infections, Feb 25-28, 2007, Los Angeles, CA.
-
Wai, J., Fisher, T., Embrey, M., Egbertson, M., Vacca, J., Hazuda, D., Miller, M., Witmer, L., Gabryelski, L., and Lyle, T. (2007) Next generation of inhibitors of HIV-1 integrase strand transfer inhibitor: structural diversity and resistance profiles, in 14 th Conference on Retroviruses and Opportunistic Infections, Feb 25-28, 2007, Los Angeles, CA.
-
(2007)
Next Generation of Inhibitors of HIV-1 Integrase Strand Transfer Inhibitor: Structural Diversity and Resistance Profiles
-
-
Wai, J.1
Fisher, T.2
Embrey, M.3
Egbertson, M.4
Vacca, J.5
Hazuda, D.6
Miller, M.7
Witmer, L.8
Gabryelski, L.9
Lyle, T.10
-
30
-
-
33644863638
-
Novel HIV-1 integrase inhibitors derived from quinolone antibiotics
-
Sato, M., Motomura, T., Aramaki, H., Matsuda, T., Yamashita, M., Ito, Y., Kawakami, H., Matsuzaki, Y., Watanabe, W., Yamataka, K., Ikeda, S., Kodama, E., Matsuoka, M., and Shinkai, H. (2006) Novel HIV-1 integrase inhibitors derived from quinolone antibiotics J. Med. Chem. 49, 1506-1508
-
(2006)
J. Med. Chem.
, vol.49
, 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
-
31
-
-
33645405333
-
Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: Design, synthesis, biological activities, and mechanism of action
-
Di Santo, R., Costi, R., Roux, A., Artico, M., Lavecchia, A., Marinelli, L., Novellino, E., Palmisano, L., Andreotti, M., Amici, R., Galluzzo, C. M., Nencioni, L., Palamara, A. T., Pommier, Y., and Marchand, C. (2006) Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action J. Med. Chem. 49, 1939-1945
-
(2006)
J. Med. Chem.
, vol.49
, pp. 1939-1945
-
-
Di Santo, R.1
Costi, R.2
Roux, A.3
Artico, M.4
Lavecchia, A.5
Marinelli, L.6
Novellino, E.7
Palmisano, L.8
Andreotti, M.9
Amici, R.10
Galluzzo, C.M.11
Nencioni, L.12
Palamara, A.T.13
Pommier, Y.14
Marchand, C.15
-
32
-
-
49449093292
-
Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: Design, synthesis, and biological activities
-
Di Santo, R., Costi, R., Roux, A., Miele, G., Crucitti, G. C., Iacovo, A., Rosi, F., Lavecchia, A., Marinelli, L., Di Giovanni, C., Novellino, E., Palmisano, L., Andreotti, M., Amici, R., Galluzzo, C. M., Nencioni, L., Palamara, A. T., Pommier, Y., and Marchand, C. (2008) Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities J. Med. Chem. 51, 4744-4750
-
(2008)
J. Med. Chem.
, vol.51
, pp. 4744-4750
-
-
Di Santo, R.1
Costi, R.2
Roux, A.3
Miele, G.4
Crucitti, G.C.5
Iacovo, A.6
Rosi, F.7
Lavecchia, A.8
Marinelli, L.9
Di Giovanni, C.10
Novellino, E.11
Palmisano, L.12
Andreotti, M.13
Amici, R.14
Galluzzo, C.M.15
Nencioni, L.16
Palamara, A.T.17
Pommier, Y.18
Marchand, C.19
-
33
-
-
20744447462
-
Recombinant HIV-1 integrase exhibits a capacity for full-site integration in vitro that is comparable to that of purified preintegration complexes from virus-infected cells
-
Sinha, S. and Grandgenett, D. P. (2005) Recombinant HIV-1 integrase exhibits a capacity for full-site integration in vitro that is comparable to that of purified preintegration complexes from virus-infected cells J. Virol. 79, 8208-8216
-
(2005)
J. Virol.
, vol.79
, pp. 8208-8216
-
-
Sinha, S.1
Grandgenett, D.P.2
-
34
-
-
44949212848
-
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors
-
Chen, X., Tsiang, M., Yu, F., Hung, M., Jones, G. S., Zeynalzadegan, A., Qi, X., Jin, H., Kim, C. U., Swaminathan, S., and Chen, J. M. (2008) Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors J. Mol. Biol. 380, 504-519
-
(2008)
J. Mol. Biol.
, vol.380
, pp. 504-519
-
-
Chen, X.1
Tsiang, M.2
Yu, F.3
Hung, M.4
Jones, G.S.5
Zeynalzadegan, A.6
Qi, X.7
Jin, H.8
Kim, C.U.9
Swaminathan, S.10
Chen, J.M.11
-
35
-
-
1842457823
-
Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions
-
Svarovskaia, E. S., Barr, R., Zhang, X., Pais, G. C., Marchand, C., Pommier, Y., Burke, T. R., Jr., and Pathak, V. K. (2004) Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions J. Virol. 78, 3210-3222
-
(2004)
J. Virol.
, vol.78
, pp. 3210-3222
-
-
Svarovskaia, E.S.1
Barr, R.2
Zhang, X.3
Pais, G.C.4
Marchand, C.5
Pommier, Y.6
Burke Jr., T.R.7
Pathak, V.K.8
-
36
-
-
67650898933
-
Pharmacovirological impact of an integrase inhibitor on human immunodeficiency virus type 1 cDNA species in vivo
-
Goffinet, C., Allespach, I., Oberbremer, L., Golden, P. L., Foster, S. A., Johns, B. A., Weatherhead, J. G., Novick, S. J., Chiswell, K. E., Garvey, E. P., and Keppler, O. T. (2009) Pharmacovirological impact of an integrase inhibitor on human immunodeficiency virus type 1 cDNA species in vivo J. Virol. 83, 7706-7717
-
(2009)
J. Virol.
, vol.83
, pp. 7706-7717
-
-
Goffinet, C.1
Allespach, I.2
Oberbremer, L.3
Golden, P.L.4
Foster, S.A.5
Johns, B.A.6
Weatherhead, J.G.7
Novick, S.J.8
Chiswell, K.E.9
Garvey, E.P.10
Keppler, O.T.11
-
37
-
-
73849095055
-
Impact of Y143 HIV-1 integrase mutations on resistance to raltegravir in vitro and in vivo
-
Delelis, O., Thierry, S., Subra, F., Simon, F., Malet, I., Alloui, C., Sayon, S., Calvez, V., Deprez, E., Marcelin, A. G., Tchertanov, L., and Mouscadet, J. F. (2010) Impact of Y143 HIV-1 integrase mutations on resistance to raltegravir in vitro and in vivo Antimicrob. Agents Chemother. 54, 491-501
-
(2010)
Antimicrob. Agents Chemother.
, vol.54
, pp. 491-501
-
-
Delelis, O.1
Thierry, S.2
Subra, F.3
Simon, F.4
Malet, I.5
Alloui, C.6
Sayon, S.7
Calvez, V.8
Deprez, E.9
Marcelin, A.G.10
Tchertanov, L.11
Mouscadet, J.F.12
-
38
-
-
0027537684
-
Comparison of DNA binding and integration half-site selection by avian myeloblastosis virus integrase
-
Grandgenett, D. P., Inman, R. B., Vora, A. C., and Fitzgerald, M. L. (1993) Comparison of DNA binding and integration half-site selection by avian myeloblastosis virus integrase J. Virol. 67, 2628-2636
-
(1993)
J. Virol.
, vol.67
, pp. 2628-2636
-
-
Grandgenett, D.P.1
Inman, R.B.2
Vora, A.C.3
Fitzgerald, M.L.4
-
39
-
-
50949119501
-
Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance
-
Zahm, J. A., Bera, S., Pandey, K. K., Vora, A., Stillmock, K., Hazuda, D., and Grandgenett, D. P. (2008) Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance Antimicrob. Agents Chemother. 52, 3358-3368
-
(2008)
Antimicrob. Agents Chemother.
, vol.52
, pp. 3358-3368
-
-
Zahm, J.A.1
Bera, S.2
Pandey, K.K.3
Vora, A.4
Stillmock, K.5
Hazuda, D.6
Grandgenett, D.P.7
-
40
-
-
0033546149
-
Multiple integrase functions are required to form the native structure of the human immunodeficiency virus type i intasome
-
Chen, H., Wei, S. Q., and Engelman, A. (1999) Multiple integrase functions are required to form the native structure of the human immunodeficiency virus type I intasome J. Biol. Chem. 274, 17358-17364
-
(1999)
J. Biol. Chem.
, vol.274
, pp. 17358-17364
-
-
Chen, H.1
Wei, S.Q.2
Engelman, A.3
-
41
-
-
61749086407
-
Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant
-
Garvey, E. P., Schwartz, B., Gartland, M. J., Lang, S., Halsey, W., Sathe, G., Carter, H. L., and Weaver, K. L. (2009) Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant Biochemistry 48, 1644-1653
-
(2009)
Biochemistry
, vol.48
, pp. 1644-1653
-
-
Garvey, E.P.1
Schwartz, B.2
Gartland, M.J.3
Lang, S.4
Halsey, W.5
Sathe, G.6
Carter, H.L.7
Weaver, K.L.8
-
42
-
-
58149154667
-
The terminal (catalytic) adenosine of the HIV LTR controls the kinetics of binding and dissociation of HIV integrase strand transfer inhibitors
-
Langley, D. R., Samanta, H. K., Lin, Z., Walker, M. A., Krystal, M. R., and Dicker, I. B. (2008) The terminal (catalytic) adenosine of the HIV LTR controls the kinetics of binding and dissociation of HIV integrase strand transfer inhibitors Biochemistry 47, 13481-13488
-
(2008)
Biochemistry
, vol.47
, pp. 13481-13488
-
-
Langley, D.R.1
Samanta, H.K.2
Lin, Z.3
Walker, M.A.4
Krystal, M.R.5
Dicker, I.B.6
-
43
-
-
70349214209
-
Slow binding inhibitors
-
in (, Ed.) pp - 177, Wiley-Interscience, New York.
-
Copeland, R. A. (2005) Slow binding inhibitors, in Evaluation of enzyme inhibitors in drug discovery (Copeland, R. A., Ed.) pp 141 - 177, Wiley-Interscience, New York.
-
(2005)
Evaluation of Enzyme Inhibitors in Drug Discovery
, pp. 141
-
-
Copeland, R.A.1
Copeland, R.A.2
-
44
-
-
33644861936
-
HIV-1 integration requires the viral DNA end (5′-C) interaction with glutamine 148 of the integrase flexible loop
-
Johnson, A. A., Santos, W., Pais, G. C., Marchand, C., Amin, R., Burke, T. R., Jr., Verdine, G., and Pommier, Y. (2006) HIV-1 integration requires the viral DNA end (5′-C) interaction with glutamine 148 of the integrase flexible loop J. Biol. Chem. 281, 461-467
-
(2006)
J. Biol. Chem.
, vol.281
, pp. 461-467
-
-
Johnson, A.A.1
Santos, W.2
Pais, G.C.3
Marchand, C.4
Amin, R.5
Burke Jr., T.R.6
Verdine, G.7
Pommier, Y.8
-
45
-
-
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, B. T., Bain, A., Thomas, C. J., and Pommier, Y. (2008) Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants Biochemistry 47, 9345-9354
-
(2008)
Biochemistry
, vol.47
, pp. 9345-9354
-
-
Marinello, J.1
Marchand, C.2
Mott, B.T.3
Bain, A.4
Thomas, C.J.5
Pommier, Y.6
-
46
-
-
14944374558
-
Integrase inhibitors to treat HIV/AIDS
-
Pommier, Y., Johnson, A. A., and Marchand, C. (2005) Integrase inhibitors to treat HIV/AIDS Nat. Rev. Drug Discov. 4, 236-248
-
(2005)
Nat. Rev. Drug Discov.
, vol.4
, pp. 236-248
-
-
Pommier, Y.1
Johnson, A.A.2
Marchand, C.3
-
47
-
-
22144486601
-
Interfacial inhibitors of protein-nucleic acid interactions
-
Pommier, Y. and Marchand, C. (2005) Interfacial inhibitors of protein-nucleic acid interactions Curr. Med. Chem. Anticancer Agents 5, 421-429
-
(2005)
Curr. Med. Chem. Anticancer Agents
, vol.5
, pp. 421-429
-
-
Pommier, Y.1
Marchand, C.2
-
48
-
-
53049101908
-
Biochemical analysis of HIV-1 integrase variants resistant to strand transfer inhibitors
-
Dicker, I. B., Terry, B., Lin, Z., Li, Z., Bollini, S., Samanta, H. K., Gali, V., Walker, M. A., and Krystal, M. R. (2008) Biochemical analysis of HIV-1 integrase variants resistant to strand transfer inhibitors J. Biol. Chem. 283, 23599-23609
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 23599-23609
-
-
Dicker, I.B.1
Terry, B.2
Lin, Z.3
Li, Z.4
Bollini, S.5
Samanta, H.K.6
Gali, V.7
Walker, M.A.8
Krystal, M.R.9
-
49
-
-
42049119625
-
Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro
-
Malet, I., Delelis, O., Valantin, M. A., Montes, B., Soulie, C., Wirden, M., Tchertanova, L., Peytavin, G., Reynes, J., Mouscadet, J. F., Katlama, C., Calvez, V., and Marcelin, A. G. (2008) Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro Antimicrob. Agents Chemother. 52, 1351-1358
-
(2008)
Antimicrob. Agents Chemother.
, vol.52
, pp. 1351-1358
-
-
Malet, I.1
Delelis, O.2
Valantin, M.A.3
Montes, B.4
Soulie, C.5
Wirden, M.6
Tchertanova, L.7
Peytavin, G.8
Reynes, J.9
Mouscadet, J.F.10
Katlama, C.11
Calvez, V.12
Marcelin, A.G.13
-
50
-
-
70349909699
-
HIV-1 in alternative molecular recognition of DNA induced by raltegravir resistance mutations
-
Mouscadet, J. F., Arora, R., Andre, J., Lambry, J. C., Delelis, O., Malet, I., Marcelin, A. G., Calvez, V., and Tchertanov, L. (2009) HIV-1 IN alternative molecular recognition of DNA induced by raltegravir resistance mutations J. Mol. Recognit. 22, 480-494
-
(2009)
J. Mol. Recognit.
, vol.22
, pp. 480-494
-
-
Mouscadet, J.F.1
Arora, R.2
Andre, J.3
Lambry, J.C.4
Delelis, O.5
Malet, I.6
Marcelin, A.G.7
Calvez, V.8
Tchertanov, L.9
-
51
-
-
77956886199
-
Resistance to HIV-1 integrase inhibitors: A structural perspective
-
(2010). (in press).
-
Mouscadet, J. F., Delelis, O., Marcelin, A. G., and Tchertanov, L. (2010) Resistance to HIV-1 integrase inhibitors: a structural perspective. Drug Resist. Update (in press).
-
Drug Resist. Update
-
-
Mouscadet, J.F.1
Delelis, O.2
Marcelin, A.G.3
Tchertanov, L.4
-
52
-
-
77951677904
-
Biochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravir
-
Metifiot, M., Maddali, K., Naumova, A., Zhang, X., Marchand, C., and Pommier, Y. (2010) Biochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravir Biochemistry 49, 3715-3722
-
(2010)
Biochemistry
, vol.49
, pp. 3715-3722
-
-
Metifiot, M.1
Maddali, K.2
Naumova, A.3
Zhang, X.4
Marchand, C.5
Pommier, Y.6
-
53
-
-
77957052689
-
-
in 10th International Workshop on Clinical Pharmacology of HIV Therapy, pp Abstract - 10, Amsterdam.
-
Grobler, J. A., McKemma, P. M., and Ly, S., and (2009) Functionally irreversible inhibition of integration by slowly dissociating strand transfer inhibitors, in 10th International Workshop on Clinical Pharmacology of HIV Therapy, pp Abstract O - 10, Amsterdam.
-
(2009)
Functionally Irreversible Inhibition of Integration by Slowly Dissociating Strand Transfer Inhibitors
-
-
Grobler, J.A.1
McKemma, P.M.2
Ly, S.3
-
54
-
-
42949114952
-
The lentiviral integrase binding protein LEDGF/p75 and HIV-1 replication
-
Engelman, A. and Cherepanov, P. (2008) The lentiviral integrase binding protein LEDGF/p75 and HIV-1 replication PLoS Pathog. 4, e1000046
-
(2008)
PLoS Pathog.
, vol.4
, pp. 1000046
-
-
Engelman, A.1
Cherepanov, P.2
-
55
-
-
77957101377
-
The interaction between lentiviral integrase and LEDGF: Structural and functional insights
-
Hare, S. and Cherepanov, P. (2009) The interaction between lentiviral integrase and LEDGF: structural and functional insights Viruses 1, 780-801
-
(2009)
Viruses
, vol.1
, pp. 780-801
-
-
Hare, S.1
Cherepanov, P.2
-
56
-
-
77957027357
-
HIV-1 integrase-DNA recognition mechanisms
-
Kessl, J., McKee, C., Eidahl, J., Shkriabai, N., Katz, A., and Kvaratskhelia, M. (2009) HIV-1 integrase-DNA recognition mechanisms Viruses 1, 713-736
-
(2009)
Viruses
, vol.1
, pp. 713-736
-
-
Kessl, J.1
McKee, C.2
Eidahl, J.3
Shkriabai, N.4
Katz, A.5
Kvaratskhelia, M.6
|