-
1
-
-
0028998825
-
The PETT series, a new class of potent nonnucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase
-
Ahgren, C., K. Backro, F. W. Bell, A. S. Cantrell, M. Clemens, J. M. Colacino, J. B. Deeter, J. A. Engelhardt, H. M., S. R. Jaskunas, N. G. Johansson, C. L. Jordan, J. S. Kasher, M. D. Kinnick, P. Lind, C. Lopez, J. M. J. Morin, M. A. Muesing, R. Noreen, B. Oberg, C. J. Paget, J. A. Palkowitz, C. A. Parrish, P. Pranc, M. K. Rippy, C. Rydergard, C. Sahlberg, S. Swanson, R. J. Ternansky, T. Unge, R. T. Vasileff, L. Vrang, S. J. West, H. Zhang, and X. X. Zhou. 1995. The PETT series, a new class of potent nonnucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. Antimicrob. Agents Chemother. 39:1329-1335.
-
(1995)
Antimicrob. Agents Chemother.
, vol.39
, pp. 1329-1335
-
-
Ahgren, C.1
Backro, K.2
Bell, F.W.3
Cantrell, A.S.4
Clemens, M.5
Colacino, J.M.6
Deeter, J.B.7
Engelhardt, J.A.8
M., H.9
Jaskunas, S.R.10
Johansson, N.G.11
Jordan, C.L.12
Kasher, J.S.13
Kinnick, M.D.14
Lind, P.15
Lopez, C.16
Morin, J.M.J.17
Muesing, M.A.18
Noreen, R.19
Oberg, B.20
Paget, C.J.21
Palkowitz, J.A.22
Parrish, C.A.23
Pranc, P.24
Rippy, M.K.25
Rydergard, C.26
Sahlberg, C.27
Swanson, S.28
Ternansky, R.J.29
Unge, T.30
Vasileff, R.T.31
Vrang, L.32
West, S.J.33
Zhang, H.34
Zhou, X.X.35
more..
-
2
-
-
0026513552
-
Highly potent and selective inhibition of HIV-1 replication by 6-phenylthiouracil derivatives
-
Baba, M., S. Shigeta, H. Tanaka, T. Miyasaka, M. Ubasawa, K. Umezu, R. T. Walker, R. Pauwels, and E. De Clercq. 1992. Highly potent and selective inhibition of HIV-1 replication by 6-phenylthiouracil derivatives. Antiviral Res. 17:245-264.
-
(1992)
Antiviral Res.
, vol.17
, pp. 245-264
-
-
Baba, M.1
Shigeta, S.2
Tanaka, H.3
Miyasaka, T.4
Ubasawa, M.5
Umezu, K.6
Walker, R.T.7
Pauwels, R.8
De Clercq, E.9
-
3
-
-
0029437758
-
Novel concepts in the treatment of human immunodeficiency virus type 1 (HIV-1) infections by HIV-1-specific reverse transcriptase inhibitors
-
Balzarini, J. 1995. Novel concepts in the treatment of human immunodeficiency virus type 1 (HIV-1) infections by HIV-1-specific reverse transcriptase inhibitors. Verh. K. Acad. Geneeskd. Belg. 57:575-600.
-
(1995)
Verh. K. Acad. Geneeskd. Belg.
, vol.57
, pp. 575-600
-
-
Balzarini, J.1
-
4
-
-
0026606044
-
2′,5′-Bis-O-(tertbutyldimethylsilyl)-3′-spiro-5″- (4″-amino-1″,2″-oxathiole-2″,2′-dioxide) pyrimidine (TSAO) nucleoside analogues: Highly selective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase
-
Balzarini, J., M. J. Perez Perez, A. San Felix, D. Schols, C. F. Perno, A. M. Vandamme, M. J. Camarasa, and E. De Clercq. 1992. 2′,5′-Bis-O-(tertbutyldimethylsilyl)-3′-spiro-5″- (4″-amino-1″,2″-oxathiole-2″,2′-dioxide) pyrimidine (TSAO) nucleoside analogues: highly selective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase. Proc. Natl. Acad. Sci. USA 89:4392-4396.
-
(1992)
Proc. Natl. Acad. Sci. USA
, vol.89
, pp. 4392-4396
-
-
Balzarini, J.1
Perez Perez, M.J.2
San Felix, A.3
Schols, D.4
Perno, C.F.5
Vandamme, A.M.6
Camarasa, M.J.7
De Clercq, E.8
-
5
-
-
0028850110
-
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs
-
Bell, F. W., A. S. Cantrell, M. Hogberg, S. R. Jaskunas, N. G. Johansson, C. L. Jordan, M. D. Kinnick, P. Lind, J. M. Morin, Jr., R. Noreen, B. Oberg, J. A. Palkowitz, C. A. Parrish, P. Pranc, C. Sahlberg, R. T. Ternansky, R. T. Vasileff, L. Vrang, S. J. West, H. Zhang, and X. X. Zhou. 1995. Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. J. Med. Chem. 38:4929-4936.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 4929-4936
-
-
Bell, F.W.1
Cantrell, A.S.2
Hogberg, M.3
Jaskunas, S.R.4
Johansson, N.G.5
Jordan, C.L.6
Kinnick, M.D.7
Lind, P.8
Morin J.M., Jr.9
Noreen, R.10
Oberg, B.11
Palkowitz, J.A.12
Parrish, C.A.13
Pranc, P.14
Sahlberg, C.15
Ternansky, R.T.16
Vasileff, R.T.17
Vrang, L.18
West, S.J.19
Zhang, H.20
Zhou, X.X.21
more..
-
6
-
-
0028454828
-
The development of a simple empirical scoring function to estimate the binding constant for a protein-ligand complex of known three-dimensional structure
-
Bohm, H. J. 1994. The development of a simple empirical scoring function to estimate the binding constant for a protein-ligand complex of known three-dimensional structure. J. Comput.-Aided Mol. Des. 8:243-256.
-
(1994)
J. Comput.-Aided Mol. Des.
, vol.8
, pp. 243-256
-
-
Bohm, H.J.1
-
7
-
-
0027027467
-
LUDI: Rule-based automatic design of new substituents for enzyme inhibitor leads
-
Bohm, H. J. 1992. LUDI: rule-based automatic design of new substituents for enzyme inhibitor leads. J. Comput.-Aided Mol. Des. 6:593-606.
-
(1992)
J. Comput.-Aided Mol. Des.
, vol.6
, pp. 593-606
-
-
Bohm, H.J.1
-
8
-
-
0024969084
-
Scintillation proximity assay
-
Bosworth, N., and P. Towers. 1989. Scintillation proximity assay. Nature 341: 167-168.
-
(1989)
Nature
, vol.341
, pp. 167-168
-
-
Bosworth, N.1
Towers, P.2
-
9
-
-
0028838466
-
Structure-activity and cross-resistance evaluations of a series of human immunodeficiency virus type 1-specific compounds related to oxathiin carboxanilide
-
Buckheit, R. W., Jr., T. L. Kinjerski, V. Fliakas-Boltz, J. D. Russell, T. L. Stup, L. A. Pallansch, W. G. Brouwer, D. C. Dao, W. A. Harrison, R. J. Schultz, J. P. Bader, and S. S. Yang. 1996. Structure-activity and cross-resistance evaluations of a series of human immunodeficiency virus type 1-specific compounds related to oxathiin carboxanilide. Antimicrob. Agents Chemother. 39:2718-2727.
-
(1996)
Antimicrob. Agents Chemother.
, vol.39
, pp. 2718-2727
-
-
Buckheit R.W., Jr.1
Kinjerski, T.L.2
Fliakas-Boltz, V.3
Russell, J.D.4
Stup, T.L.5
Pallansch, L.A.6
Brouwer, W.G.7
Dao, D.C.8
Harrison, W.A.9
Schultz, R.J.10
Bader, J.P.11
Yang, S.S.12
-
10
-
-
18544400158
-
Efficacy, pharmacokinetics, and in vivo antiviral activity of UC781, a highly potent, orally bioavailable nonnucleoside reverse transcriptase inhibitor of HIV type 1
-
Buckheit, R. W., Jr., M. Hollingshead, S. Stinson, V. Fliakas-Boltz, L. A. Pallansch, J. Roberson, W. Decker, C. Elder, S. Borgel, C. Bonomi, R. Shores, T. Siford, L. Malspeis, and J. P. Bader. 1997. Efficacy, pharmacokinetics, and in vivo antiviral activity of UC781, a highly potent, orally bioavailable nonnucleoside reverse transcriptase inhibitor of HIV type 1. AIDS Res. Hum. Retroviruses 13:789-796.
-
(1997)
AIDS Res. Hum. Retroviruses
, vol.13
, pp. 789-796
-
-
Buckheit R.W., Jr.1
Hollingshead, M.2
Stinson, S.3
Fliakas-Boltz, V.4
Pallansch, L.A.5
Roberson, J.6
Decker, W.7
Elder, C.8
Borgel, S.9
Bonomi, C.10
Shores, R.11
Siford, T.12
Malspeis, L.13
Bader, J.P.14
-
11
-
-
8244226649
-
Highly potent oxathiin carboxanilide derivatives with efficacy against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus isolates
-
Buckheit, R. W., Jr., M. J. Snow, V. Fliakas-Boltz, T. L. Kinjerski, J. D. Russell, L. A. Pallansch, W. G. Brouwer, and S. S. Yang. 1997. Highly potent oxathiin carboxanilide derivatives with efficacy against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus isolates. Antimicrob. Agents Chemother. 41:831-837.
-
(1997)
Antimicrob. Agents Chemother.
, vol.41
, pp. 831-837
-
-
Buckheit R.W., Jr.1
Snow, M.J.2
Fliakas-Boltz, V.3
Kinjerski, T.L.4
Russell, J.D.5
Pallansch, L.A.6
Brouwer, W.G.7
Yang, S.S.8
-
12
-
-
10244222420
-
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs
-
Cantrell, A. S., P. Engelhardt, M. Hogberg, S. R. Jaskunas, N. G. Johansson, C. L. Jordan, J. Kangasmetsa, M. D. Kinnick, P. Lind, J. M. Morin, Jr., M. A. Muesing, R. Noreen, B. Oberg, P. Pranc, C. Sahlberg, R. J. Ternansky, R. T. Vasileff, L. Vrang, S. J. West, and H. Zhang. 1996. Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs. J. Med. Chem. 39:4261-4274.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 4261-4274
-
-
Cantrell, A.S.1
Engelhardt, P.2
Hogberg, M.3
Jaskunas, S.R.4
Johansson, N.G.5
Jordan, C.L.6
Kangasmetsa, J.7
Kinnick, M.D.8
Lind, P.9
Morin J.M., Jr.10
Muesing, M.A.11
Noreen, R.12
Oberg, B.13
Pranc, P.14
Sahlberg, C.15
Ternansky, R.J.16
Vasileff, R.T.17
Vrang, L.18
West, S.J.19
Zhang, H.20
more..
-
13
-
-
0021107965
-
Solvent-accessible surfaces of proteins and nucleic acids
-
Connolly, M. L. 1983. Solvent-accessible surfaces of proteins and nucleic acids. Science 221:709-713.
-
(1983)
Science
, vol.221
, pp. 709-713
-
-
Connolly, M.L.1
-
14
-
-
0029939554
-
Synthesis and potent anti-HIV-1 activity of novel 6-benzyluracil analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine
-
Danel, K., E. Larsen, E. B. Pedersen, B. F. Vestergaard, and C. Nielsen. 1996. Synthesis and potent anti-HIV-1 activity of novel 6-benzyluracil analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. J. Med. Chem. 39:2427-2431.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2427-2431
-
-
Danel, K.1
Larsen, E.2
Pedersen, E.B.3
Vestergaard, B.F.4
Nielsen, C.5
-
15
-
-
0031086857
-
Anti-HIV active naphthyl analogues of HEPT and DABO
-
Danel, K., C. Nielsen, and E. B. Pedersen. 1997. Anti-HIV active naphthyl analogues of HEPT and DABO. Acta Chem. Scand. 51:426-430.
-
(1997)
Acta Chem. Scand.
, vol.51
, pp. 426-430
-
-
Danel, K.1
Nielsen, C.2
Pedersen, E.B.3
-
16
-
-
0031942724
-
Synthesis and anti-HIV-1 activity of novel 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones
-
Danel, K., E. B. Pedersen, and C. Nielsen. 1998. Synthesis and anti-HIV-1 activity of novel 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones. J. Med. Chem. 41:191-198.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 191-198
-
-
Danel, K.1
Pedersen, E.B.2
Nielsen, C.3
-
17
-
-
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., J. Ding, Y. Hsiou, A. D. Clark, Jr., H. Moereels, L. Koymans, K. Andries, R. Pauwels, P. A. Janssen, P. L. Boyer, P. Clark, R. H. Smith, Jr., M. B. Kroeger Smith, C. J. Michejda, S. H. Hughes, and E. Arnold. 1996. 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. 264:1085-1100.
-
(1996)
J. Mol. Biol.
, vol.264
, pp. 1085-1100
-
-
Das, K.1
Ding, J.2
Hsiou, Y.3
Clark A.D., Jr.4
Moereels, H.5
Koymans, L.6
Andries, K.7
Pauwels, R.8
Janssen, P.A.9
Boyer, P.L.10
Clark, P.11
Smith R.H., Jr.12
Kroeger Smith, M.B.13
Michejda, C.J.14
Hughes, S.H.15
Arnold, E.16
-
19
-
-
0029011730
-
Toward improved anti-HIV chemotherapy: Therapeutic strategies for intervention with HIV infections
-
De Clercq, E. 1995. Toward improved anti-HIV chemotherapy: therapeutic strategies for intervention with HIV infections. J. Med. Chem. 38:2491-2517.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 2491-2517
-
-
De Clercq, E.1
-
20
-
-
0029075207
-
Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors
-
Ding, J., K. Das, H. Moereels, L. Koymans, K. Andries, P. A. Janssen, S. H. Hughes, and E. Arnold. 1995. Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nat. Struct. Biol. 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.6
Hughes, S.H.7
Arnold, E.8
-
21
-
-
0029644484
-
Structure of HIV-1 reverse transcriptase in a complex with the non-nucleoside inhibitor alpha-APA R 95845 at 2.8 A resolution
-
Ding, J., K. Das, C. Tantillo, W. Zhang, A. D. Clark, Jr., S. Jessen, X. Lu, Y. Hsiou, A. Jacobo Molina, K. Andries, R. Pauwels, H. Moereels, L. Koymans, P. A. J. Janssen, R. H. J. Smith, R. Kroeger Koepke, C. J. Michejda, S. H. Hughes, and E. Arnold. 1995. Structure of HIV-1 reverse transcriptase in a complex with the non-nucleoside inhibitor alpha-APA R 95845 at 2.8 A resolution. Structure 3:365-379.
-
(1995)
Structure
, vol.3
, pp. 365-379
-
-
Ding, J.1
Das, K.2
Tantillo, C.3
Zhang, W.4
Clark A.D., Jr.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, R.H.J.15
Kroeger Koepke, R.16
Michejda, C.J.17
Hughes, S.H.18
Arnold, E.19
-
22
-
-
0027515958
-
Anti-human immunodeficiency virus type 1 activity of an anti-CD4 immumiconjugate containing pokeweed antiviral protein
-
Erice, A., H. H. Balfour, Jr., D. E. Myers, V. L. Leske, K. J. Sannerud, V. Kuebelbeck, J. D. Irvin, and F. M. Uckun. 1993. Anti-human immunodeficiency virus type 1 activity of an anti-CD4 immumiconjugate containing pokeweed antiviral protein. Antimicrob. Agents Chemother. 37:835-838.
-
(1993)
Antimicrob. Agents Chemother.
, vol.37
, pp. 835-838
-
-
Erice, A.1
Balfour H.H., Jr.2
Myers, D.E.3
Leske, V.L.4
Sannerud, K.J.5
Kuebelbeck, V.6
Irvin, J.D.7
Uckun, F.M.8
-
23
-
-
0030935265
-
Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U-90152 explain resistance mutations for this nonnucleoside inhibitor
-
Esnouf, R. M., J. Ren, A. L. Hopkins, C. K. Ross, E. Y. Jones, D. K. Stammers, and D. I. Stuart. 1997. Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U-90152 explain resistance mutations for this nonnucleoside inhibitor. Proc. Natl. Acad. Sci. USA 94:3984-3989.
-
(1997)
Proc. Natl. Acad. Sci. USA
, vol.94
, pp. 3984-3989
-
-
Esnouf, R.M.1
Ren, J.2
Hopkins, A.L.3
Ross, C.K.4
Jones, E.Y.5
Stammers, D.K.6
Stuart, D.I.7
-
24
-
-
8244230512
-
Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives
-
Font, M., A. Monge, E. Alvarez, A. Cuartero, M. J. Losa, M. J. Fidalgo, C. SanMartin, E. Nadal, I. Ruiz, I. Merino, J. J. Martinez-Irujo, E. Alberdi, E. Santiago, I. Prieto, J. J. Lasarte, P. Sarobe, and F. Borras. 1997. Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives. Drug Des. Discovery 14: 305-332.
-
(1997)
Drug Des. Discovery
, vol.14
, pp. 305-332
-
-
Font, M.1
Monge, A.2
Alvarez, E.3
Cuartero, A.4
Losa, M.J.5
Fidalgo, M.J.6
Sanmartin, C.7
Nadal, E.8
Ruiz, I.9
Merino, I.10
Martinez-Irujo, J.J.11
Alberdi, E.12
Santiago, E.13
Prieto, I.14
Lasarte, J.J.15
Sarobe, P.16
Borras, F.17
-
25
-
-
0030976265
-
Thiadiazole derivatives: Highly potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replications in vitro
-
Fujiwara, M., K. Ijichi, Y. Hanasaki, T. Ide, K. Katsuura, H. Takayama, N. Aimi, S. Shigeta, K. Konno, T. Yokota, and M. Baba. 1997. Thiadiazole derivatives: highly potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replications in vitro. Microbiol. Immunol. 41: 301-308.
-
(1997)
Microbiol. Immunol.
, vol.41
, pp. 301-308
-
-
Fujiwara, M.1
Ijichi, K.2
Hanasaki, Y.3
Ide, T.4
Katsuura, K.5
Takayama, H.6
Aimi, N.7
Shigeta, S.8
Konno, K.9
Yokota, T.10
Baba, M.11
-
26
-
-
0025968569
-
The molecular biology of human immunodeficiency virus tvpe 1 infections
-
Greene, W. C. 1991. The molecular biology of human immunodeficiency virus tvpe 1 infections. N. Engl. J. Med. 324:308-317.
-
(1991)
N. Engl. J. Med.
, vol.324
, pp. 308-317
-
-
Greene, W.C.1
-
27
-
-
0026607918
-
Nonnucleoside inhibitors of HIV-1 reverse transcriptase: Nevirapine as a prototype drug
-
Grob, P. M., J. C. Wu, K. A. Cohen, R. H. Ingraham, C. K. Shih, K. D. Hargrave, T. L. McTague, and V. J. Merluzzi. 1992. Nonnucleoside inhibitors of HIV-1 reverse transcriptase: nevirapine as a prototype drug. AIDS Res. Hum. Retroviruses 8:145-152.
-
(1992)
AIDS Res. Hum. Retroviruses
, vol.8
, pp. 145-152
-
-
Grob, P.M.1
Wu, J.C.2
Cohen, K.A.3
Ingraham, R.H.4
Shih, C.K.5
Hargrave, K.D.6
McTague, T.L.7
Merluzzi, V.J.8
-
28
-
-
0030983790
-
The inhibitory activity of diazinyl-substituted thiourea derivatives on human immunodeficiency virus type 1 reverse transcriptase
-
Heinisch, G., B. Matuszczak, S. Pachler, and D. Rakowitz. 1997. The inhibitory activity of diazinyl-substituted thiourea derivatives on human immunodeficiency virus type 1 reverse transcriptase. Antiviral Chem. Chemother. 8: 443-446.
-
(1997)
Antiviral Chem. Chemother.
, vol.8
, pp. 443-446
-
-
Heinisch, G.1
Matuszczak, B.2
Pachler, S.3
Rakowitz, D.4
-
29
-
-
0029976422
-
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors
-
Hopkins, A. L., J. Ren, R. M. Esnouf, B. E. Willcox, E. Y. Jones, C. Ross, T. Miyasaka, R. T. Walker, H. Tanaka, D. K. Stammers, and D. I. Stuart. 1996. Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors. J. Med. Chem. 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
-
-
84889120137
-
Improved methods for binding protein models in electron density maps and the location of errors in these models
-
Jones, T. A., J. Y. Zou, S. W. Cowan, and G. Kjeldgaard. 1991. Improved methods for binding protein models in electron density maps and the location of errors in these models. Acta Crystallogr. A 47:110-119.
-
(1991)
Acta Crystallogr. A
, vol.47
, pp. 110-119
-
-
Jones, T.A.1
Zou, J.Y.2
Cowan, S.W.3
Kjeldgaard, G.4
-
31
-
-
0030070683
-
Selective pressure of a quinoxaline nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) on HIV-1 replication results in the emergence of nucleoside RT-inhibitor-specific (RT Leu-74→Val or Ile and Val-75→Leu or Ile) HIV-1 mutants
-
Kleim, J. P., M. Rosner, I. Winkler, A. Paessens, R. Kirsch, Y. Hsiou, E. Arnold, and G. Riess. 1996. Selective pressure of a quinoxaline nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) on HIV-1 replication results in the emergence of nucleoside RT-inhibitor-specific (RT Leu-74→Val or Ile and Val-75→Leu or Ile) HIV-1 mutants. Proc. Natl. Acad. Sci. USA 93:34-38.
-
(1996)
Proc. Natl. Acad. Sci. USA
, vol.93
, pp. 34-38
-
-
Kleim, J.P.1
Rosner, M.2
Winkler, I.3
Paessens, A.4
Kirsch, R.5
Hsiou, Y.6
Arnold, E.7
Riess, G.8
-
32
-
-
0026693137
-
Crystal structure at 3.5 a resolution of HIV-1 reverse transcriptase complexed with an inhibitor
-
Kohlstaedt, L. A., J. Wang, J. M. Friedman, P. A. Rice, and T. A. Steitz. 1992. Crystal structure at 3.5 A resolution of HIV-1 reverse transcriptase complexed with an inhibitor. Science 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
-
33
-
-
84986511247
-
A molecular mechanics/grid method for evaluation of ligand-receptor interactions
-
Luty, B. A., P. F. Wasserman, P. F. Stouten, C. N. Hodge, M. Zacharias, and J. A. McCammon. 1995. A molecular mechanics/grid method for evaluation of ligand-receptor interactions. J. Comp. Chem. 16:454-464.
-
(1995)
J. Comp. Chem.
, vol.16
, pp. 454-464
-
-
Luty, B.A.1
Wasserman, P.F.2
Stouten, P.F.3
Hodge, C.N.4
Zacharias, M.5
McCammon, J.A.6
-
34
-
-
15444340492
-
Dihydro(alkylthio)(n-aphthylmethyl)oxopyrimidines: Novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series
-
Mai, A., M. Artica, G. Sbardella, S. Quartarone, S. Massa, A. G. Loi, A. D. Montis, F. Scintu, M. Putzolu, and P. La Colla. 1997. Dihydro(alkylthio)(n-aphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. J. Med. Chem. 40:1447-1454.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 1447-1454
-
-
Mai, A.1
Artica, M.2
Sbardella, G.3
Quartarone, S.4
Massa, S.5
Loi, A.G.6
Montis, A.D.7
Scintu, F.8
Putzolu, M.9
La Colla, P.10
-
35
-
-
0032544145
-
Structure-based design of N-[2-(1-piperidinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
-
Mao, C., R. Vig, T. K. Venkatachalam, E. A. Sudbeck, and F. M. Uckun. 1998. Structure-based design of N-[2-(1-piperidinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. Bioorg. Med. Chem. Lett. 8:2213-2218.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 2213-2218
-
-
Mao, C.1
Vig, R.2
Venkatachalam, T.K.3
Sudbeck, E.A.4
Uckun, F.M.5
-
36
-
-
0025186450
-
Molecular targets for AIDS therapy
-
Mitsuya, H., R. Yarchoan, and S. Broder. 1990. Molecular targets for AIDS therapy. Science 249:1533-1544.
-
(1990)
Science
, vol.249
, pp. 1533-1544
-
-
Mitsuya, H.1
Yarchoan, R.2
Broder, S.3
-
37
-
-
0342384817
-
-
Molecular Simulations Inc., San Diego, Calif.
-
Molecular Simulations Inc. 1996. InsightII. Molecular Simulations Inc., San Diego, Calif.
-
(1996)
InsightII
-
-
-
39
-
-
0030994577
-
Synthesis and anti-HIV activity of novel N-1 side chain-modified analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)
-
Pontikis, R., R. Benhida, A. M. Aubertin, D. S. Grierson, and C. Monneret. 1997. Synthesis and anti-HIV activity of novel N-1 side chain-modified analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). J. Med. Chem. 40:1845-1854.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 1845-1854
-
-
Pontikis, R.1
Benhida, R.2
Aubertin, A.M.3
Grierson, D.S.4
Monneret, C.5
-
40
-
-
0028947588
-
High resolution structures of HIV-1 RT from four RT-inhihitor complexes
-
Ken, J., R. Esnouf, E. Garman, D. Somers, C. Ross, I. Kirby, J. Keeling, G. Darby, Y. Jones, D. Stuart, and D. Stammers. 1995. High resolution structures of HIV-1 RT from four RT-inhihitor complexes. Nat. Struct. Biol. 2: 293-302.
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 293-302
-
-
Ken, J.1
Esnouf, R.2
Garman, E.3
Somers, D.4
Ross, C.5
Kirby, I.6
Keeling, J.7
Darby, G.8
Jones, Y.9
Stuart, D.10
Stammers, D.11
-
41
-
-
0029645409
-
The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: Lessons for inhibitor design
-
Ren, J., R. Esnouf, A. Hopkins, C. Ross, Y. Jones, D. Stammers, and D. Stuart. 1995. The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: lessons for inhibitor design. Structure 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
-
42
-
-
0027278282
-
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: Structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3-[(1-methylethyl) amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate
-
Romero, D. L., R. A. Morge, M. J. Genin, C. Biles, M. Busso, L. Resnick, I. W. Althaus, F. Reusser, R. C. Thomas, and W. G. Tarpley. 1993. Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3-[(1-methylethyl) amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate. J. Med. Chem. 36:1505-1508.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 1505-1508
-
-
Romero, D.L.1
Morge, R.A.2
Genin, M.J.3
Biles, C.4
Busso, M.5
Resnick, L.6
Althaus, I.W.7
Reusser, F.8
Thomas, R.C.9
Tarpley, W.G.10
-
43
-
-
9544229686
-
Targeting delavirdine/ atevirdine resistant HIV-1: Identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors
-
Romero, D. L., R. A. Olmsted, T. J. Poel, R. A. Morge, C. Biles, B. J. Keiser, L. A. Kopta, J. M. Friis, J. D. Hosley, K. J. Stefanski, D. G. Wishka, D. B. Evans, J. Morris, R. G. Stehle, S. K. Sharma, Y. Yagi, R. L. Voorman, W. J. Adams, W. G. Tarpley, and R. C. Thomas. 1996. Targeting delavirdine/ atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. J. Med. Them. 39:3769-3789.
-
(1996)
J. Med. Them.
, vol.39
, pp. 3769-3789
-
-
Romero, D.L.1
Olmsted, R.A.2
Poel, T.J.3
Morge, R.A.4
Biles, C.5
Keiser, B.J.6
Kopta, L.A.7
Friis, J.M.8
Hosley, J.D.9
Stefanski, K.J.10
Wishka, D.G.11
Evans, D.B.12
Morris, J.13
Stehle, R.G.14
Sharma, S.K.15
Yagi, Y.16
Voorman, R.L.17
Adams, W.J.18
Tarpley, W.G.19
Thomas, R.C.20
more..
-
44
-
-
0028271687
-
Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1
-
Smerdon, S. J., J. Jager, J. Wang, L. A. Kohlstaedt, A. J. Chirino, J. M. Friedman, P. A. Rice, and T. A. Steitz. 1994. Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1. Proc. Natl. Acad. Sci. USA 91:3911-3915.
-
(1994)
Proc. Natl. Acad. Sci. USA
, vol.91
, pp. 3911-3915
-
-
Smerdon, S.J.1
Jager, J.2
Wang, J.3
Kohlstaedt, L.A.4
Chirino, A.J.5
Friedman, J.M.6
Rice, P.A.7
Steitz, T.A.8
-
45
-
-
0026071537
-
A new class of HIV-1-specific 6-substituted acyclouridine derivatives: Synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)
-
Tanaka, H., M. Baba, H. Hayakawa, T. Sakamaki, T. Miyasaka, M. Ubasawa, H. Takashima, K. Sekiya, I. Nitta, S. Shigeta, R. T. Walker, J. Balzarini, and E. De Clercq. 1991. A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5-or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). J. Med. Chem. 34:349-357.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 349-357
-
-
Tanaka, H.1
Baba, M.2
Hayakawa, H.3
Sakamaki, T.4
Miyasaka, T.5
Ubasawa, M.6
Takashima, H.7
Sekiya, K.8
Nitta, I.9
Shigeta, S.10
Walker, R.T.11
Balzarini, J.12
De Clercq, E.13
-
46
-
-
0028172345
-
Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Implications for mechanisms of drug inhibition and resistance
-
Tantillo, C., J. Ding, A. Jacobo Molina, R. G. Nanni, P. L. Boyer, S. H. Hughes, R. Pauwels, K. Andries, P. A. Janssen, and E. Arnold. 1994. Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Implications for mechanisms of drug inhibition and resistance. J. Mol. Biol. 243:369-387.
-
(1994)
J. Mol. Biol.
, vol.243
, pp. 369-387
-
-
Tantillo, C.1
Ding, J.2
Jacobo Molina, A.3
Nanni, R.G.4
Boyer, P.L.5
Hughes, S.H.6
Pauwels, R.7
Andries, K.8
Janssen, P.A.9
Arnold, E.10
-
47
-
-
0031943905
-
TXU (anti-CD7)-pokeweed antiviral protein as a potent inhibitor of human immunodeficiency virus
-
Uckun, F. M., L. M. Chelstrom, L. Tuel-Ahlgren, I. Dibirdik, J. D. Irvin, M. Chandan-Langlie, and D. E. Myers. 1998. TXU (anti-CD7)-pokeweed antiviral protein as a potent inhibitor of human immunodeficiency virus. Antimicrob. Agents Chemother. 42:383-388.
-
(1998)
Antimicrob. Agents Chemother.
, vol.42
, pp. 383-388
-
-
Uckun, F.M.1
Chelstrom, L.M.2
Tuel-Ahlgren, L.3
Dibirdik, I.4
Irvin, J.D.5
Chandan-Langlie, M.6
Myers, D.E.7
-
48
-
-
0031788490
-
Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase
-
Vig, R., C. Mao, T. K. Venkatachalan, L. Tuel-Ahlgren, E. A. Sudbeck, and F. M. Uckun. 1998. Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase. Bioorg. Med. Chem. 6:1-9.
-
(1998)
Bioorg. Med. Chem.
, vol.6
, pp. 1-9
-
-
Vig, R.1
Mao, C.2
Venkatachalan, T.K.3
Tuel-Ahlgren, L.4
Sudbeck, E.A.5
Uckun, F.M.6
-
49
-
-
0025126625
-
+ cells by monoclonal antibodies
-
+ cells by monoclonal antibodies. Nature 347:92-95.
-
(1990)
Nature
, vol.347
, pp. 92-95
-
-
Zarling, J.M.1
Moran, P.A.2
Haffar, O.3
Sias, J.4
Richman, D.D.5
Spina, C.A.6
Myers, D.E.7
Kuebelbeck, V.8
Ledbetter, J.A.9
Uckun, F.M.10
|