-
1
-
-
40449097507
-
The medicinal chemistry of the DATA and DAPY series of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)
-
Heeres, J. and Lewi, P.J. (2007) The medicinal chemistry of the DATA and DAPY series of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Advances in Antiviral Drug Design, 5, 213-242.
-
(2007)
Advances in Antiviral Drug Design
, vol.5
, pp. 213-242
-
-
Heeres, J.1
Lewi, P.J.2
-
2
-
-
0023687234
-
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds
-
Pauwels, R., Balzarini, J., Baba, M., Snoeck, R., Schols, D., Herdewijn, P., Desmyter, J., and De Clercq, E. (1988) Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. Journal of Virological Methods, 20, 309-321.
-
(1988)
Journal of Virological Methods
, vol.20
, pp. 309-321
-
-
Pauwels, R.1
Balzarini, J.2
Baba, M.3
Snoeck, R.4
Schols, D.5
Herdewijn, P.6
Desmyter, J.7
De Clercq, E.8
-
3
-
-
40749129190
-
Tetrazolium-based colorimetric assay for the detection ofHIV replication inhibitors: revisited 20 years later
-
Pannecouque, C., Daelemans, D., and De Clercq, E. (2008) Tetrazolium-based colorimetric assay for the detection ofHIV replication inhibitors: revisited 20 years later. Nature Protocols, 3, 427-434.
-
(2008)
Nature Protocols
, vol.3
, pp. 427-434
-
-
Pannecouque, C.1
Daelemans, D.2
De Clercq, E.3
-
4
-
-
0025014499
-
Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives
-
Pauwels, R., Andries, K., Desmyter, J., Schols, D., Kukla, M.J., Breslin, H.J., Raeymaeckers, A., Van Gelder, J., Woestenborghs, R., Heykants, J., Schellekens, K., Janssen, M.A.C., De Clercq, E., and Janssen, P.A.J. (1990) Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature, 343, 470-474.
-
(1990)
Nature
, vol.343
, pp. 470-474
-
-
Pauwels, R.1
Andries, K.2
Desmyter, J.3
Schols, D.4
Kukla, M.J.5
Breslin, H.J.6
Raeymaeckers, A.7
Van Gelder, J.8
Woestenborghs, R.9
Heykants, J.10
Schellekens, K.11
Janssen, M.A.C.12
De Clercq, E.13
Janssen, P.A.J.14
-
5
-
-
0025973691
-
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives
-
Kukla, M.J., Breslin, H.J., Pauwels, R., Fedde, C.L., Miranda, M., Scott, M.K., Sherrill, R.G., Raeymaekers, A., Van Gelder, J., Andries, K., Janssen, M.A.C., De Clercq, E., and Janssen, P.A.J. (1991) Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. Journal ofMedicinal Chemistry, 34, 746-751.
-
(1991)
Journal ofMedicinal Chemistry
, vol.34
, pp. 746-751
-
-
Kukla, M.J.1
Breslin, H.J.2
Pauwels, R.3
Fedde, C.L.4
Miranda, M.5
Scott, M.K.6
Sherrill, R.G.7
Raeymaekers, A.8
Van Gelder, J.9
Andries, K.10
Janssen, M.A.C.11
De Clercq, E.12
Janssen, P.A.J.13
-
6
-
-
0026347180
-
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methyl-imidazo [4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives
-
Kukla, M.J., Breslin, H.J., Diamond, C.J., Grous, P.P., Ho, C.Y., Miranda, M., Rodgers, J.D., Sherrill, R.G., De Clercq, E., Pauwels, R., Andries, K., Moens, L.J., Janssen, M.A.C., and Janssen, P.A.J. (1991) Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methyl-imidazo [4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. Journal of Medicinal Chemistry, 34, 3187-3197.
-
(1991)
Journal of Medicinal Chemistry
, vol.34
, pp. 3187-3197
-
-
Kukla, M.J.1
Breslin, H.J.2
Diamond, C.J.3
Grous, P.P.4
Ho, C.Y.5
Miranda, M.6
Rodgers, J.D.7
Sherrill, R.G.8
De Clercq, E.9
Pauwels, R.10
Andries, K.11
Moens, L.J.12
Janssen, M.A.C.13
Janssen, P.A.J.14
-
7
-
-
0036050539
-
Strategies in the design of antiviral drugs
-
De Clercq, E. (2002) Strategies in the design of antiviral drugs. Nature Reviews. Drug Discovery, 1, 13-25.
-
(2002)
Nature Reviews. Drug Discovery
, vol.1
, pp. 13-25
-
-
De Clercq, E.1
-
8
-
-
0028172345
-
Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase
-
Tantillo, C., Ding, J., Jacobo-Molina, A., Nanni, R.G., Boyer, P.L., Hughes, S.H., Pauwels, R., Andries, K., Janssen, P.A., and Arnold, E. (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. Journal of Molecular Biology, 243, 369-387.
-
(1994)
Implications for mechanisms of drug inhibition and resistance. Journal of Molecular Biology
, 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
-
9
-
-
0025962924
-
An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives
-
Debyser, Z., Pauwels, R., Andries, K., Desmyter, J., Kukla, M., Janssen, P.A., and De Clercq, E. (1991) An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives. Proceedings of the National Academy of Sciences of the United States of America, 88, 1451-1455.
-
(1991)
Proceedings of the National Academy of Sciences of the United States of America
, vol.88
, pp. 1451-1455
-
-
Debyser, Z.1
Pauwels, R.2
Andries, K.3
Desmyter, J.4
Kukla, M.5
Janssen, P.A.6
De Clercq, E.7
-
10
-
-
0027447133
-
HIV-1-specific RT inhibitors: highly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase
-
De Clercq, E. (1993) HIV-1-specific RT inhibitors: highly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase. Medicinal Research Reviews, 13, 229-258.
-
(1993)
Medicinal Research Reviews
, vol.13
, pp. 229-258
-
-
De Clercq, E.1
-
11
-
-
0029775166
-
What can be expected from non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the treatment of human immunodeficiency virus type 1 (HIV-1) infections?
-
De Clercq, E. (1996) What can be expected from non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the treatment of human immunodeficiency virus type 1 (HIV-1) infections? Reviews in Medical Virology, 6, 97-117.
-
(1996)
Reviews in Medical Virology
, vol.6
, pp. 97-117
-
-
De Clercq, E.1
-
12
-
-
0032437454
-
The role of nonnucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection
-
De Clercq, E. (1998) The role of nonnucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection. Antiviral Research, 38, 153-179.
-
(1998)
Antiviral Research
, vol.38
, pp. 153-179
-
-
De Clercq, E.1
-
13
-
-
12144265244
-
Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future
-
De Clercq, E. (2004) Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future. Chemistry & Biodiversity, 1, 44-64.
-
(2004)
Chemistry & Biodiversity
, vol.1
, pp. 44-64
-
-
De Clercq, E.1
-
14
-
-
57349120749
-
The discovery of antiviral agents: ten different compounds, ten different stories
-
De Clercq, E. (2008) The discovery of antiviral agents: ten different compounds, ten different stories. Medicinal Research Reviews, 28, 929-953.
-
(2008)
Medicinal Research Reviews
, vol.28
, pp. 929-953
-
-
De Clercq, E.1
-
15
-
-
0027407551
-
Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of a-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase
-
Pauwels, R., Andries, K., Debyser, Z., Van Daele, P., Schols, D., Stoffels, P., De Vreese, K., Woestenborghs, R., Vandamme, A.-M., Janssen, C.G.M., Anne, J., Cauwenbergh, G., Desmyter, J., Heykants, J., Janssen, M.A.C., De Clercq, E., and Janssen, P.A.J. (1993) Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of a-anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Proceedings of the National Academy of Sciences of the United States of America, 90, 1711-1715.
-
(1993)
Proceedings of the National Academy of Sciences of the United States of America
, vol.90
, pp. 1711-1715
-
-
Pauwels, R.1
Andries, K.2
Debyser, Z.3
Van Daele, P.4
Schols, D.5
Stoffels, P.6
De Vreese, K.7
Woestenborghs, R.8
Vandamme, A.-M.9
Janssen, C.G.M.10
Anne, J.11
Cauwenbergh, G.12
Desmyter, J.13
Heykants, J.14
Janssen, M.A.C.15
De Clercq, E.16
Janssen, P.A.J.17
-
16
-
-
17944376896
-
Evolution of anti-HIV drug candidates
-
Ludovici, D.W., Kukla, M.J., Grous, P.G., Krishnan, S., Andries, K., de Bethune, M.-P., Azijn, H., Pauwels, R., De Clercq, E., Arnold, E., and Janssen, P.A.J. (2001) Evolution of anti-HIV drug candidates. Part 1: from a-anilinophenylacetamide (a-APA) to imidoyl thiourea (ITU). Bioorganic & Medicinal Chemistry Letters, 11, 2225-2228.
-
(2001)
Part 1: from a-anilinophenylacetamide (a-APA) to imidoyl thiourea (ITU). Bioorganic & Medicinal Chemistry Letters
, vol.11
, pp. 2225-2228
-
-
Ludovici, D.W.1
Kukla, M.J.2
Grous, P.G.3
Krishnan, S.4
Andries, K.5
de Bethune, M.-P.6
Azijn, H.7
Pauwels, R.8
De Clercq, E.9
Arnold, E.10
Janssen, P.A.J.11
-
17
-
-
17944366732
-
Evolution of anti-HIV drug candidates
-
Ludovici, D.W., Kavash, R.W., Kukla, M.J., Ho, C.Y., Ye, H., De Corte, B.L., Andries, K., de Bethune, M.P., Azijn, H., Pauwels, R., Moereels, H.E., Heeres, J., Koymans, L.M., de Jonge, M.R., Van Aken, K.J., Daeyaert, F.F., Lewi, P.J., Das, K., Arnold, E., and Janssen, P.A. (2001) Evolution of anti-HIV drug candidates. Part 2: diaryltriazine (DATA) analogues. Bioorganic & Medicinal Chemistry Letters, 11, 2229-2234.
-
(2001)
Part 2: diaryltriazine (DATA) analogues. Bioorganic & Medicinal Chemistry Letters
, vol.11
, pp. 2229-2234
-
-
Ludovici, D.W.1
Kavash, R.W.2
Kukla, M.J.3
Ho, C.Y.4
Ye, H.5
De Corte, B.L.6
Andries, K.7
de Bethune, M.P.8
Azijn, H.9
Pauwels, R.10
Moereels, H.E.11
Heeres, J.12
Koymans, L.M.13
de Jonge, M.R.14
Van Aken, K.J.15
Daeyaert, F.F.16
Lewi, P.J.17
Das, K.18
Arnold, E.19
Janssen, P.A.20
more..
-
18
-
-
17944374798
-
Evolution of anti-HIV drug candidates
-
Ludovici, D.W., De Corte, B.L., Kukla, M.J., Ye, H., Ho, C.Y., Lichtenstein, M.A., Kavash, R.W., Andries, K., de Bethune, M.P., Azijn, H., Pauwels, R., Lewi, P.J., Heeres, J., Koymans, L.M., de Jonge, M.R., Van Aken, K.J., Daeyaert, F.F., Das, K., Arnold, E., and Janssen, P.A. (2001) Evolution of anti-HIV drug candidates. Part 3: diarylpyrimidine (DAPY) analogues. Bioorganic & Medicinal Chemistry Letters, 11, 2235-2239.
-
(2001)
Part 3: diarylpyrimidine (DAPY) analogues. Bioorganic & Medicinal Chemistry Letters
, vol.11
, pp. 2235-2239
-
-
Ludovici, D.W.1
De Corte, B.L.2
Kukla, M.J.3
Ye, H.4
Ho, C.Y.5
Lichtenstein, M.A.6
Kavash, R.W.7
Andries, K.8
de Bethune, M.P.9
Azijn, H.10
Pauwels, R.11
Lewi, P.J.12
Heeres, J.13
Koymans, L.M.14
de Jonge, M.R.15
Van Aken, K.J.16
Daeyaert, F.F.17
Das, K.18
Arnold, E.19
Janssen, P.A.20
more..
-
19
-
-
9644291579
-
TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1
-
Andries, K., Azijn, H., Thielemans, T., Ludovici, D., Kukla, M., Heeres, J., Janssen, P., De Corte, B., Vingerhoets, J., Pauwels, R., and de Bethune, M.P. (2004) TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrobial Agents and Chemotherapy, 48, 4680-4686.
-
(2004)
Antimicrobial Agents and Chemotherapy
, vol.48
, pp. 4680-4686
-
-
Andries, K.1
Azijn, H.2
Thielemans, T.3
Ludovici, D.4
Kukla, M.5
Heeres, J.6
Janssen, P.7
De Corte, B.8
Vingerhoets, J.9
Pauwels, R.10
de Bethune, M.P.11
-
20
-
-
20144372481
-
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]-benzonitrile (R278474, rilpivirine)
-
Janssen, P.A., Lewi, P.J., Arnold, E., Daeyaert, F., de Jonge, M., Heeres, J., Koymans, L., Vinkers, M., Guillemont, J., Pasquier, E., Kukla, M., Ludovici, D., Andries, K., de Bethune, M.P., Pauwels, R., Das, K., Clark, A.D., Jr., Frenkel, Y.V., Hughes, S.H., Medaer, B., De Knaep, F., Bohets, H., De Clerck, F., Lampo, A., Williams, P., and Stoffels, P. (2005) In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]-benzonitrile (R278474, rilpivirine). Journal ofMedicinal Chemistry, 48, 1901-1909.
-
(2005)
Journal ofMedicinal Chemistry
, vol.48
, pp. 1901-1909
-
-
Janssen, P.A.1
Lewi, P.J.2
Arnold, E.3
Daeyaert, F.4
de Jonge, M.5
Heeres, J.6
Koymans, L.7
Vinkers, M.8
Guillemont, J.9
Pasquier, E.10
Kukla, M.11
Ludovici, D.12
Andries, K.13
de Bethune, M.P.14
Pauwels, R.15
Das, K.16
Clark, Jr.A.D.17
Frenkel, Y.V.18
Hughes, S.H.19
Medaer, B.20
De Knaep, F.21
Bohets, H.22
De Clerck, F.23
Lampo, A.24
Williams, P.25
Stoffels, P.26
more..
-
21
-
-
75749118495
-
TMC278, a next-generation NNRTI, active against wild-type and NNRTIresistant HIV-1
-
Azijn, H, Tirry, I., Vingerhoets, J., de Bethune, M.P., Kraus, G., Boven, K., Jochmans, D., Van Craenenbroeck, E., Picchio, G., and Rimsky, L.T. (2010) TMC278, a next-generation NNRTI, active against wild-type and NNRTIresistant HIV-1. Antimicrobial Agents and Chemotherapy, 54, 718-727.
-
(2010)
Antimicrobial Agents and Chemotherapy
, vol.54
, pp. 718-727
-
-
Azijn, H.1
Tirry, I.2
Vingerhoets, J.3
de Bethune, M.P.4
Kraus, G.5
Boven, K.6
Jochmans, D.7
Van Craenenbroeck, E.8
Picchio, G.9
Rimsky, L.T.10
-
22
-
-
0029075207
-
Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors
-
Ding, J., Das, K., Moereels, H., Koymans, L., Andries, K., Janssen, P.A., Hughes, S.H., and Arnold, E. (1995) Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nature Structural Biology, 2, 407-415.
-
(1995)
Nature Structural Biology
, 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
-
23
-
-
9744258219
-
Crystallography and the design of anti-AIDS drugs: conformational flexibility and positional adaptability are important in the design of non-nucleoside HIV-1 reverse transcriptase inhibitors
-
Das, K., Lewi, P.J., Hughes, S.H., and Arnold, E. (2005) Crystallography and the design of anti-AIDS drugs: conformational flexibility and positional adaptability are important in the design of non-nucleoside HIV-1 reverse transcriptase inhibitors. Progress in Biophysics & Molecular Biology, 88, 209-231.
-
(2005)
Progress in Biophysics & Molecular Biology
, vol.88
, pp. 209-231
-
-
Das, K.1
Lewi, P.J.2
Hughes, S.H.3
Arnold, E.4
-
24
-
-
40349094606
-
Twodimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase
-
Fang, C., Bauman, J.D., Das, K., Remorino, A., Arnold, E., and Hochstrasser, R.M. (2008) Twodimensional infrared spectra reveal relaxation of the nonnucleoside inhibitor TMC278 complexed with HIV-1 reverse transcriptase. Proceedings of the National Academy of Sciences of the United States of America, 105, 1472-1477.
-
(2008)
Proceedings of the National Academy of Sciences of the United States of America
, vol.105
, pp. 1472-1477
-
-
Fang, C.1
Bauman, J.D.2
Das, K.3
Remorino, A.4
Arnold, E.5
Hochstrasser, R.M.6
-
25
-
-
40349091258
-
Highresolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations
-
Das, K., Bauman, J.D., Clark, A.D., Jr., Frenkel, Y.V., Lewi, P.J., Shatkin, A.J., Hughes, S.H., and Arnold, E. (2008)Highresolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations. Proceedings of the National Academy of Sciences of the United States of America, 105, 1466-1471.
-
(2008)
Proceedings of the National Academy of Sciences of the United States of America
, vol.105
, pp. 1466-1471
-
-
Das, K.1
Bauman, J.D.2
Clark, Jr.A.D.3
Frenkel, Y.V.4
Lewi, P.J.5
Shatkin, A.J.6
Hughes, S.H.7
Arnold, E.8
-
26
-
-
0031463691
-
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase
-
Roth, T., Morningstar, M.L., Boyer, P.L., Hughes, S.H., Buckheit, R.W., Jr., and Michejda, C.J. (1997) Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles. Journal of Medicinal Chemistry, 40, 4199-4207.
-
(1997)
2-Aryl-substituted benzimidazoles. Journal of Medicinal Chemistry
, vol.40
, pp. 4199-4207
-
-
Roth, T.1
Morningstar, M.L.2
Boyer, P.L.3
Hughes, S.H.4
Buckheit, Jr.R.W.5
Michejda, C.J.6
-
27
-
-
34548128318
-
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme
-
Morningstar, M.L., Roth, T., Farnsworth, D.W., Smith, M.K., Watson, K., Buckheit, R.W., Jr., Das, K., Zhang, W., Arnold, E., Julias, J.G., Hughes, S.H., and Michejda, C.J. (2007) Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme. Journal of Medicinal Chemistry, 50, 4003-4015.
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, pp. 4003-4015
-
-
Morningstar, M.L.1
Roth, T.2
Farnsworth, D.W.3
Smith, M.K.4
Watson, K.5
Buckheit, Jr.R.W.6
Das, K.7
Zhang, W.8
Arnold, E.9
Julias, J.G.10
Hughes, S.H.11
Michejda, C.J.12
-
28
-
-
50849105061
-
Crystal engineering of HIV-1 reverse transcriptase for structure-based drug design
-
Bauman, J.D., Das, K., Ho, W.C., Baweja, M., Himmel, D.M., Clark, A.D., Jr., Oren, D.A., Boyer, P.L., Hughes, S.H., Shatkin, A.J., and Arnold, E. (2008) Crystal engineering of HIV-1 reverse transcriptase for structure-based drug design. Nucleic Acids Research, 36, 5083-5092.
-
(2008)
Nucleic Acids Research
, vol.36
, pp. 5083-5092
-
-
Bauman, J.D.1
Das, K.2
Ho, W.C.3
Baweja, M.4
Himmel, D.M.5
Clark, Jr.A.D.6
Oren, D.A.7
Boyer, P.L.8
Hughes, S.H.9
Shatkin, A.J.10
Arnold, E.11
-
29
-
-
70350043532
-
Conformational landscape of the human immunodeficiency virus type 1 reverse transcriptase non-nucleoside inhibitor binding pocket: lessons for inhibitor design from a cluster analysis of many crystal structures
-
Paris, K.A., Haq, O., Felts, A.K., Das, K., Arnold, E., and Levy, R.M. (2009) Conformational landscape of the human immunodeficiency virus type 1 reverse transcriptase non-nucleoside inhibitor binding pocket: lessons for inhibitor design from a cluster analysis of many crystal structures. Journal of Medicinal Chemistry, 52, 6413-6420.
-
(2009)
Journal of Medicinal Chemistry
, vol.52
, pp. 6413-6420
-
-
Paris, K.A.1
Haq, O.2
Felts, A.K.3
Das, K.4
Arnold, E.5
Levy, R.M.6
-
30
-
-
70349650215
-
Molecular dynamics study of non-nucleoside reverse transcriptase inhibitor 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethylphenyl] amino]-2-pyrimidinyl]amino]benzonitrile (TMC278/rilpivirine) aggregates: correlation between amphiphilic properties of the drug and oral bioavailability
-
Frenkel, YV., Gallicchio, E., Das, K., Levy, RM., and Arnold, E. (2009) Molecular dynamics study of non-nucleoside reverse transcriptase inhibitor 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethylphenyl] amino]-2-pyrimidinyl]amino]benzonitrile (TMC278/rilpivirine) aggregates: correlation between amphiphilic properties of the drug and oral bioavailability. Journal of Medicinal Chemistry, 52, 5896-5905.
-
(2009)
Journal of Medicinal Chemistry
, vol.52
, pp. 5896-5905
-
-
Frenkel, YV.1
Gallicchio, E.2
Das, K.3
Levy, RM.4
Arnold, E.5
-
31
-
-
34248397581
-
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains
-
Mordant, C., Schmitt, B., Pasquier, E., Demestre, C., Queguiner, L.,Masungi, C., Peeters, A., Smeulders, L., Bettens, E., Hertogs, K., Heeres, J., Lewi, P., and Guillemont, J. (2007) Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains. European Journal of Medicinal Chemistry, 42, 567-579.
-
(2007)
European Journal of Medicinal Chemistry
, vol.42
, pp. 567-579
-
-
Mordant, C.1
Schmitt, B.2
Pasquier, E.3
Demestre, C.4
Queguiner, L.5
Masungi, C.6
Peeters, A.7
Smeulders, L.8
Bettens, E.9
Hertogs, K.10
Heeres, J.11
Lewi, P.12
Guillemont, J.13
-
32
-
-
55049101937
-
Powder for reconstitution of the anti-HIV-1 drug TMC278: formulation development, stability and animal studies
-
Van Gyseghem, E., Pendela, M., Baert, L., Rosier, J., Van't Klooster, G., De Man, H., Bouche, M.P., Schueller, L., Van Remoortere, P., Wigerinck, P., Adams, E., Hoogmartens, J., and Van Den Mooter, G. (2008) Powder for reconstitution of the anti-HIV-1 drug TMC278: formulation development, stability and animal studies. The European Journal of Pharmaceutics and Biopharmaceutics, 70, 853-860.
-
(2008)
The European Journal of Pharmaceutics and Biopharmaceutics
, vol.70
, pp. 853-860
-
-
Van Gyseghem, E.1
Pendela, M.2
Baert, L.3
Rosier, J.4
Van't Klooster, G.5
De Man, H.6
Bouche, M.P.7
Schueller, L.8
Van Remoortere, P.9
Wigerinck, P.10
Adams, E.11
Hoogmartens, J.12
Van Den Mooter, G.13
-
33
-
-
59449097782
-
Development of a liquid chromatographic assay for an anti-HIV tablet containing lamivudine, zidovudine and TMC278.HCL
-
Pendela, M., Van Gyseghem, E., Van Den Mooter, G., Baert, L., Rosier, J., Hoogmartens, J., and Adams, E. (2009) Development of a liquid chromatographic assay for an anti-HIV tablet containing lamivudine, zidovudine and TMC278.HCL. Journal of Pharmaceutical and Biomedical Analysis, 49, 508-512.
-
(2009)
Journal of Pharmaceutical and Biomedical Analysis
, vol.49
, pp. 508-512
-
-
Pendela, M.1
Van Gyseghem, E.2
Van Den Mooter, G.3
Baert, L.4
Rosier, J.5
Hoogmartens, J.6
Adams, E.7
-
34
-
-
67449119172
-
Development of a long-acting injectable formulation with nanoparticles of rilpivirine (TMC278) for HIV treatment
-
Baert, L., van't Klooster, G., Dries, W., François, M., Wouters, A., Basstanie, E., Iterbeke, K., Stappers, F., Stevens, P., Schueller, L., Van Remoortere, P., Kraus, G., Wigerinck, P., and Rosier, J. (2009) Development of a long-acting injectable formulation with nanoparticles of rilpivirine (TMC278) for HIV treatment. European Journal of Pharmaceutics and Biopharmaceutics, 72, 502-508.
-
(2009)
European Journal of Pharmaceutics and Biopharmaceutics
, vol.72
, pp. 502-508
-
-
Baert, L.1
Van't Klooster, G.2
Dries, W.3
François, M.4
Wouters, A.5
Basstanie, E.6
Iterbeke, K.7
Stappers, F.8
Stevens, P.9
Schueller, L.10
Van Remoortere, P.11
Kraus, G.12
Wigerinck, P.13
Rosier, J.14
-
35
-
-
33748036988
-
Shortterm antiviral activity of TMC278 -a novel NNRTI -in treatment-naive HIV-1-infected subjects
-
Goebel, F., Yakovlev, A., Pozniak, A.L., Vinogradova, E., Boogaerts, G., Hoetelmans, R., de Bethune, M.P., Peeters, M., andWoodfall, B. (2006) Shortterm antiviral activity of TMC278 -a novel NNRTI -in treatment-naive HIV-1-infected subjects. AIDS (London, England), 20, 1721-1726.
-
(2006)
AIDS (London, England)
, vol.20
, pp. 1721-1726
-
-
Goebel, F.1
Yakovlev, A.2
Pozniak, A.L.3
Vinogradova, E.4
Boogaerts, G.5
Hoetelmans, R.6
de Bethune, M.P.7
Peeters, M.8
Woodfall, B.9
-
36
-
-
69849087563
-
Short-term randomized proofof-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy
-
Arasteh, K., Rieger, A., Yeni, P., Pozniak, A., Boogaerts, G., van Heeswijk, R., de Bethune, M.P., Peeters, M., andWoodfall, B. (2009) Short-term randomized proofof-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy. Antiviral Therapy, 14, 713-722.
-
(2009)
Antiviral Therapy
, vol.14
, pp. 713-722
-
-
Arasteh, K.1
Rieger, A.2
Yeni, P.3
Pozniak, A.4
Boogaerts, G.5
van Heeswijk, R.6
de Bethune, M.P.7
Peeters, M.8
andWoodfall, B.9
-
37
-
-
45949100482
-
How developing world concerns need to be part of drug development plans: a case study of four emerging antiretrovirals
-
van Roey, J., von Schoen-Angerer, T., Ford, N., and Calmy, A. (2008) How developing world concerns need to be part of drug development plans: a case study of four emerging antiretrovirals. Drug Discovery Today, 13, 601-605.
-
(2008)
Drug Discovery Today
, vol.13
, pp. 601-605
-
-
van Roey, J.1
von Schoen-Angerer, T.2
Ford, N.3
Calmy, A.4
-
38
-
-
73649148381
-
Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a phase IIb randomized trial
-
Pozniak, A.L., Morales-Ramirez, J., Katabira, E., Steyn, D., Lupo, S.H., Santoscoy, M., Grinsztejn, B., Ruxrungtham, K., Rimsky, L.T., Vanveggel, S., Boven, K.and TMC278-C204 Study Group (2010) Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a phase IIb randomized trial. AIDS (London, England), 24, 55-65.
-
(2010)
AIDS (London, England)
, vol.24
, pp. 55-65
-
-
Pozniak, A.L.1
Morales-Ramirez, J.2
Katabira, E.3
Steyn, D.4
Lupo, S.H.5
Santoscoy, M.6
Grinsztejn, B.7
Ruxrungtham, K.8
Rimsky, L.T.9
Vanveggel, S.10
Boven, K.11
-
39
-
-
73549087233
-
Pharmacokinetics and drug-drug interactions of antiretrovirals: an update
-
Dickinson, L., Khoo, S., and Back, D. (2010) Pharmacokinetics and drug-drug interactions of antiretrovirals: an update. Antiviral Research, 85, 176-189.
-
(2010)
Antiviral Research
, vol.85
, pp. 176-189
-
-
Dickinson, L.1
Khoo, S.2
Back, D.3
-
40
-
-
33444469632
-
TMC278, a new potent NNRTI, with an increased barrier to resistance and favourable pharmacokinetic profile
-
Boston, MA, USA, Abstract 556.
-
de Bethune, M.P., Andries, K., Azijn, H., Guillemont, J., Heeres, J., Vingerhoets, J., Lewi, P., Lee, E., Timmerman, P., and Williams, P. (2005) TMC278, a new potent NNRTI, with an increased barrier to resistance and favourable pharmacokinetic profile. 12th Conference on Retroviruses and Opportunistic Infections (CROI), Boston, MA, USA, Abstract 556.
-
(2005)
12th Conference on Retroviruses and Opportunistic Infections (CROI)
-
-
de Bethune, M.P.1
Andries, K.2
Azijn, H.3
Guillemont, J.4
Heeres, J.5
Vingerhoets, J.6
Lewi, P.7
Lee, E.8
Timmerman, P.9
Williams, P.10
-
41
-
-
73549083973
-
The effect of TMC278, a next generation NNRTI, on CYP3A activity in vivo
-
Amsterdam, The Netherlands, Abstract
-
Crauwels, H.M., van Heeswijk, R.P.G., Stevens, T., Stevens, M., Buelens, A., Boven, K., and Hoetelmans, R.M.W. (2009) The effect of TMC278, a next generation NNRTI, on CYP3A activity in vivo. 10th International Workshop on Clinical Pharmacology of HIV Therapy, Amsterdam, The Netherlands, Abstract P28.
-
(2009)
10th International Workshop on Clinical Pharmacology of HIV Therapy
, pp. 28
-
-
Crauwels, H.M.1
van Heeswijk, R.P.G.2
Stevens, T.3
Stevens, M.4
Buelens, A.5
Boven, K.6
Hoetelmans, R.M.W.7
-
42
-
-
73549116628
-
Pharmacokinetic interaction between the novel non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC278 and tenofovir disoproxil fumarate (TDF) in healthy volunteers
-
Rio de Janeiro, Brazil, Abstract WePe3.3C15.
-
Hoetelmans, R., Kestens, D., Stevens, M., Peeters, M., Williams, P., Bastiaanse, L., Buffels, R., and Woodfall, B. (2005) Pharmacokinetic interaction between the novel non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC278 and tenofovir disoproxil fumarate (TDF) in healthy volunteers. 3rd International AIDS Society Conference on HIV Pathogenesis and Treatment, Rio de Janeiro, Brazil, Abstract WePe3.3C15.
-
(2005)
3rd International AIDS Society Conference on HIV Pathogenesis and Treatment
-
-
Hoetelmans, R.1
Kestens, D.2
Stevens, M.3
Peeters, M.4
Williams, P.5
Bastiaanse, L.6
Buffels, R.7
Woodfall, B.8
-
43
-
-
73549106929
-
TMC278, a nextgeneration NNRTI, does not alter the pharmacokinetics of sildenafil
-
Amsterdam, The Netherlands, Abstract
-
Crauwels, H.M., van Heeswijk, R.P.G., Stevens, M., Buelens, A., Boven, K., and Hoetelmans, R. (2009) TMC278, a nextgeneration NNRTI, does not alter the pharmacokinetics of sildenafil. 10th International Workshop on Clinical Pharmacology of HIV Therapy, Amsterdam, The Netherlands, Abstract P22.
-
(2009)
10th International Workshop on Clinical Pharmacology of HIV Therapy
, pp. 22
-
-
Crauwels, H.M.1
van Heeswijk, R.P.G.2
Stevens, M.3
Buelens, A.4
Boven, K.5
Hoetelmans, R.6
-
44
-
-
61849143798
-
Compilation and prevalence of mutations associated with resistance to nonnucleoside reverse transcriptase inhibitors
-
Tambuyzer, L., Azijn, H., Rimsky, L.T., Vingerhoets, J., Lecocq, P., Kraus, G., Picchio, G., and de Bethune, M.P. (2009) Compilation and prevalence of mutations associated with resistance to nonnucleoside reverse transcriptase inhibitors. Antiviral Therapy, 14, 103-109.
-
(2009)
Antiviral Therapy
, vol.14
, pp. 103-109
-
-
Tambuyzer, L.1
Azijn, H.2
Rimsky, L.T.3
Vingerhoets, J.4
Lecocq, P.5
Kraus, G.6
Picchio, G.7
de Bethune, M.P.8
-
45
-
-
26444595584
-
TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments
-
Vingerhoets, J., Azijn, H., Fransen, E., De Baere, I., Smeulders, L., Jochmans, D., Andries, K., Pauwels, R., and de Bethune, M.P. (2005) TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. Journal of Virology, 79, 12773-12782.
-
(2005)
Journal of Virology
, vol.79
, pp. 12773-12782
-
-
Vingerhoets, J.1
Azijn, H.2
Fransen, E.3
De Baere, I.4
Smeulders, L.5
Jochmans, D.6
Andries, K.7
Pauwels, R.8
de Bethune, M.P.9
-
46
-
-
46749104685
-
Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: the development pipeline and recent clinical data
-
Sweeney, Z.K. and Klumpp, K. (2008) Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: the development pipeline and recent clinical data. Current Opinion in Drug Discovery & Development, 11, 458-470.
-
(2008)
Current Opinion in Drug Discovery & Development
, vol.11
, pp. 458-470
-
-
Sweeney, Z.K.1
Klumpp, K.2
-
47
-
-
48349089312
-
Rilpivirine, a non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection
-
Ripamonti, D. and Maggiolo, F. (2008) Rilpivirine, a non-nucleoside reverse transcriptase inhibitor for the treatment of HIV infection. Current Opinion in Investigational Drugs, 9, 899-912.
-
(2008)
Current Opinion in Investigational Drugs
, vol.9
, pp. 899-912
-
-
Ripamonti, D.1
Maggiolo, F.2
-
48
-
-
62549083388
-
Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents
-
Fulco, P.P. and McNicholl, I.R. (2009) Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents. Pharmacotherapy, 29, 281-294.
-
(2009)
Pharmacotherapy
, vol.29
, pp. 281-294
-
-
Fulco, P.P.1
McNicholl, I.R.2
-
49
-
-
67650456668
-
Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor
-
Garvey, L. and Winston, A. (2009) Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor. Expert Opinion on Investigational Drugs, 18, 1035-1041.
-
(2009)
Expert Opinion on Investigational Drugs
, vol.18
, pp. 1035-1041
-
-
Garvey, L.1
Winston, A.2
|