-
1
-
-
84875010204
-
Molecular basis of human immunodeficiency virus type 1 drug resistance: Overview and recent developments
-
L. Menéndez-Arias Molecular basis of human immunodeficiency virus type 1 drug resistance: Overview and recent developments Antiviral Res. 2013 98 93 120
-
(2013)
Antiviral Res.
, vol.98
, pp. 93-120
-
-
Menéndez-Arias, L.1
-
2
-
-
73549088708
-
Molecular basis of human immunodeficiency virus drug resistance: An update
-
L. Menéndez-Arias Molecular basis of human immunodeficiency virus drug resistance: an update Antiviral Res. 2010 85 210 231
-
(2010)
Antiviral Res.
, vol.85
, pp. 210-231
-
-
Menéndez-Arias, L.1
-
3
-
-
33750808446
-
The pharmacology of HIV drug resistance
-
M. M. Zdanowicz The pharmacology of HIV drug resistance Am. J. Pharm. Educ. 2006 70 100
-
(2006)
Am. J. Pharm. Educ.
, vol.70
, pp. 100
-
-
Zdanowicz, M.M.1
-
4
-
-
84880054656
-
HIV-1 reverse transcriptase and antiviral drug resistance. Part 1
-
K. Das E. Arnold HIV-1 reverse transcriptase and antiviral drug resistance. Part 1 Curr. Opin. Virol. 2013 3 111 118
-
(2013)
Curr. Opin. Virol.
, vol.3
, pp. 111-118
-
-
Das, K.1
Arnold, E.2
-
5
-
-
84880058866
-
HIV-1 reverse transcriptase and antiviral drug resistance. Part 2
-
K. Das E. Arnold HIV-1 reverse transcriptase and antiviral drug resistance. Part 2 Curr. Opin. Virol. 2013 3 119 128
-
(2013)
Curr. Opin. Virol.
, vol.3
, pp. 119-128
-
-
Das, K.1
Arnold, E.2
-
6
-
-
84866325636
-
Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors
-
E. L. Asahchop M. A. Wainberg R. D. Sloan C. L. Tremblay Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors Antimicrob. Agents Chemother. 2012 56 5000 5008
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 5000-5008
-
-
Asahchop, E.L.1
Wainberg, M.A.2
Sloan, R.D.3
Tremblay, C.L.4
-
7
-
-
84870824536
-
HIV-1 reverse transcriptase still remains a new drug target: Structure, function, classical inhibitors, and new inhibitors with innovative mechanisms of actions
-
F. Esposito A. Corona E. Tramontano HIV-1 reverse transcriptase still remains a new drug target: structure, function, classical inhibitors, and new inhibitors with innovative mechanisms of actions Mol. Biol. Int. 2012 2012 586401
-
(2012)
Mol. Biol. Int.
, vol.2012
, pp. 586401
-
-
Esposito, F.1
Corona, A.2
Tramontano, E.3
-
9
-
-
0033988951
-
Lethal mutagenesis of HIV by mutagenic ribonucleoside analogs
-
L. A. Loeb J. I. Mullins Lethal mutagenesis of HIV by mutagenic ribonucleoside analogs AIDS Res. Hum. Retroviruses 2000 16 1 3
-
(2000)
AIDS Res. Hum. Retroviruses
, vol.16
, pp. 1-3
-
-
Loeb, L.A.1
Mullins, J.I.2
-
11
-
-
70350291512
-
5-Azacytidine can induce lethal mutagenesis in human immunodeficiency virus type 1
-
M. J. Dapp C. L. Clouser S. Patterson L. M. Mansky 5-Azacytidine can induce lethal mutagenesis in human immunodeficiency virus type 1 J. Virol. 2009 83 11950 11958
-
(2009)
J. Virol.
, vol.83
, pp. 11950-11958
-
-
Dapp, M.J.1
Clouser, C.L.2
Patterson, S.3
Mansky, L.M.4
-
14
-
-
70350066155
-
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase
-
M. D. Cullen W. C. Ho J. D. Bauman K. Das E. Arnold T. L. Hartman K. M. Watson R. W. Buckheit C. Pannecouque E. De Clercq M. Cushman Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase J. Med. Chem. 2009 52 6467 6473
-
(2009)
J. Med. Chem.
, vol.52
, pp. 6467-6473
-
-
Cullen, M.D.1
Ho, W.C.2
Bauman, J.D.3
Das, K.4
Arnold, E.5
Hartman, T.L.6
Watson, K.M.7
Buckheit, R.W.8
Pannecouque, C.9
De Clercq, E.10
Cushman, M.11
-
15
-
-
77956705389
-
Cosalane and Its Analogues: A Unique Class of Anti-HIV Agents
-
P. Zhan Z. Li X. Liu Cosalane and Its Analogues: A Unique Class of Anti-HIV Agents Mini-Rev. Med. Chem. 2010 10 966 976
-
(2010)
Mini-Rev. Med. Chem.
, vol.10
, pp. 966-976
-
-
Zhan, P.1
Li, Z.2
Liu, X.3
-
16
-
-
79955434216
-
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide- thymine (TSAO-T) complexed with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket
-
K. Das J. D. Bauman A. S. Rim C. Dharia A. D. Clark Jr. M. J. Camarasa J. Balzarini E. Arnold Crystal structure of tert-butyldimethylsilyl- spiroaminooxathioledioxide-thymine (TSAO-T) complexed with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket J. Med. Chem. 2011 54 2727 2737
-
(2011)
J. Med. Chem.
, vol.54
, pp. 2727-2737
-
-
Das, K.1
Bauman, J.D.2
Rim, A.S.3
Dharia, C.4
Clark, Jr.A.D.5
Camarasa, M.J.6
Balzarini, J.7
Arnold, E.8
-
17
-
-
3242657912
-
Structure of HIV-1 reverse transcriptase bound to an inhibitor active against mutant reverse transcriptases resistant to other nonnucleoside inhibitors
-
J. D. Pata W. G. Stirtan S. W. Goldstein T. A. Steitz Structure of HIV-1 reverse transcriptase bound to an inhibitor active against mutant reverse transcriptases resistant to other nonnucleoside inhibitors Proc. Natl. Acad. Sci. U. S. A. 2004 101 10548 10553
-
(2004)
Proc. Natl. Acad. Sci. U. S. A.
, vol.101
, pp. 10548-10553
-
-
Pata, J.D.1
Stirtan, W.G.2
Goldstein, S.W.3
Steitz, T.A.4
-
18
-
-
79952146488
-
HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate
-
G. Maga M. Radi M. A. Gerard M. Botta E. Ennifar HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate Viruses 2010 2 880 899
-
(2010)
Viruses
, vol.2
, pp. 880-899
-
-
Maga, G.1
Radi, M.2
Gerard, M.A.3
Botta, M.4
Ennifar, E.5
-
19
-
-
34249715422
-
Discovery of non-nucleoside inhibitors of HIV-1 reverse transcriptase competing with the nucleotide substrate
-
G. Maga M. Radi S. Zanoli F. Manetti R. Cancio U. Hübscher S. Spadari C. Falciani M. Terrazas J. Vilarrasa M. Botta Discovery of non-nucleoside inhibitors of HIV-1 reverse transcriptase competing with the nucleotide substrate Angew. Chem., Int. Ed. 2007 46 1810 1813
-
(2007)
Angew. Chem., Int. Ed.
, vol.46
, pp. 1810-1813
-
-
Maga, G.1
Radi, M.2
Zanoli, S.3
Manetti, F.4
Cancio, R.5
Hübscher, U.6
Spadari, S.7
Falciani, C.8
Terrazas, M.9
Vilarrasa, J.10
Botta, M.11
-
20
-
-
47249122173
-
A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs
-
M. Radi C. Falciani L. Contemori E. Petricci G. Maga A. Samuele S. Zanoli M. Terrazas M. Castria A. Togninelli J. A. Esté I. Clotet-Codina M. Armand-Ugón M. Botta A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs ChemMedChem 2008 3 573 593
-
(2008)
ChemMedChem
, vol.3
, pp. 573-593
-
-
Radi, M.1
Falciani, C.2
Contemori, L.3
Petricci, E.4
Maga, G.5
Samuele, A.6
Zanoli, S.7
Terrazas, M.8
Castria, M.9
Togninelli, A.10
Esté, J.A.11
Clotet-Codina, I.12
Armand-Ugón, M.13
Botta, M.14
-
21
-
-
77749264656
-
Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of action
-
S. Freisz G. Bec M. Radi P. Wolff E. Crespan L. Angeli P. Dumas G. Maga M. Botta E. Ennifar Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of action Angew. Chem., Int. Ed. 2010 49 1805 1808
-
(2010)
Angew. Chem., Int. Ed.
, vol.49
, pp. 1805-1808
-
-
Freisz, S.1
Bec, G.2
Radi, M.3
Wolff, P.4
Crespan, E.5
Angeli, L.6
Dumas, P.7
Maga, G.8
Botta, M.9
Ennifar, E.10
-
22
-
-
84903791249
-
-
PCT Int. Appl., WO 2011073959 A2
-
M. Radi, M. Botta, L. Angeli, P. Wolff, E. Crespan, L. Angeli, P. Dumas, G. Maga, M. Botta and E. Ennifar, Crystal structure of HIV-1 reverse transcriptase bound to a nucleotide-competitive reverse transcriptase inhibitor and it use for the design and identification of inhibitors, PCT Int. Appl., WO 2011073959 A2, 2011
-
(2011)
Crystal Structure of HIV-1 Reverse Transcriptase Bound to A Nucleotide-competitive Reverse Transcriptase Inhibitor and It Use for the Design and Identification of Inhibitors
-
-
Radi, M.1
Botta, M.2
Angeli, L.3
Wolff, P.4
Crespan, E.5
Angeli, L.6
Dumas, P.7
Maga, G.8
Botta, M.9
Ennifar, E.10
-
23
-
-
33746883932
-
Novel nonnucleoside inhibitors that select nucleoside inhibitor resistance mutations in human immunodeficiency virus type 1 reverse transcriptase
-
Z. Zhang M. Walker W. Xu J. H. Shim J. L. Girardet R. K. Hamatake Z. Hong Novel nonnucleoside inhibitors that select nucleoside inhibitor resistance mutations in human immunodeficiency virus type 1 reverse transcriptase Antimicrob. Agents Chemother. 2006 50 2772 2781
-
(2006)
Antimicrob. Agents Chemother.
, vol.50
, pp. 2772-2781
-
-
Zhang, Z.1
Walker, M.2
Xu, W.3
Shim, J.H.4
Girardet, J.L.5
Hamatake, R.K.6
Hong, Z.7
-
24
-
-
33845410116
-
Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action
-
D. Jochmans J. Deval B. Kesteleyn H. Van Marck E. Bettens I. De Baere P. Dehertogh T. Ivens M. Van Ginderen B. Van Schoubroeck M. Ehteshami P. Wigerinck M. Götte K. Hertogs Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action J. Virol. 2006 80 12283 12292
-
(2006)
J. Virol.
, vol.80
, pp. 12283-12292
-
-
Jochmans, D.1
Deval, J.2
Kesteleyn, B.3
Van Marck, H.4
Bettens, E.5
De Baere, I.6
Dehertogh, P.7
Ivens, T.8
Van Ginderen, M.9
Van Schoubroeck, B.10
Ehteshami, M.11
Wigerinck, P.12
Götte, M.13
Hertogs, K.14
-
26
-
-
84879045198
-
Formation of a Quaternary Complex of HIV-1 Reverse Transcriptase with a Nucleotide-competing Inhibitor and its ATP Enhancer
-
M. Ehteshami M. Nijhuis J. A. Bernatchez C. J. Ablenas S. McCormick D. de Jong D. Jochmans M. Götte Formation of a Quaternary Complex of HIV-1 Reverse Transcriptase with a Nucleotide-competing Inhibitor and its ATP Enhancer J. Biol. Chem. 2013 288 17336 17346
-
(2013)
J. Biol. Chem.
, vol.288
, pp. 17336-17346
-
-
Ehteshami, M.1
Nijhuis, M.2
Bernatchez, J.A.3
Ablenas, C.J.4
McCormick, S.5
De Jong, D.6
Jochmans, D.7
Götte, M.8
-
27
-
-
84876158501
-
Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors
-
M. Tremblay R. C. Bethell M. G. Cordingley P. Deroy J. Duan M. Duplessis P. J. Edwards A. M. Faucher T. Halmos C. A. James C. Kuhn J. É. Lacoste L. Lamorte S. R. Laplante E. Malenfant J. Minville L. Morency S. Morin D. Rajotte P. Salois B. Simoneau S. Tremblay C. F. Sturino Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors Bioorg. Med. Chem. Lett. 2013 23 2775 2780
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 2775-2780
-
-
Tremblay, M.1
Bethell, R.C.2
Cordingley, M.G.3
Deroy, P.4
Duan, J.5
Duplessis, M.6
Edwards, P.J.7
Faucher, A.M.8
Halmos, T.9
James, C.A.10
Kuhn, C.11
Lacoste, J.É.12
Lamorte, L.13
Laplante, S.R.14
Malenfant, E.15
Minville, J.16
Morency, L.17
Morin, S.18
Rajotte, D.19
Salois, P.20
Simoneau, B.21
Tremblay, S.22
Sturino, C.F.23
more..
-
28
-
-
84876101790
-
Nucleotide competing reverse transcriptase inhibitors: Discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors
-
C. A. James P. Deroy M. Duplessis P. J. Edwards T. Halmos J. Minville L. Morency S. Morin B. Simoneau M. Tremblay R. Bethell M. Cordingley J. Duan L. Lamorte A. Pelletier D. Rajotte P. Salois S. Tremblay C. F. Sturino Nucleotide competing reverse transcriptase inhibitors: Discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors Bioorg. Med. Chem. Lett. 2013 23 2781 2786
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 2781-2786
-
-
James, C.A.1
Deroy, P.2
Duplessis, M.3
Edwards, P.J.4
Halmos, T.5
Minville, J.6
Morency, L.7
Morin, S.8
Simoneau, B.9
Tremblay, M.10
Bethell, R.11
Cordingley, M.12
Duan, J.13
Lamorte, L.14
Pelletier, A.15
Rajotte, D.16
Salois, P.17
Tremblay, S.18
Sturino, C.F.19
-
29
-
-
84877847712
-
Identification and characterization of a novel HIV-1 nucleotide competing RT inhibitor series
-
D. Rajotte S. Tremblay A. Pelletier P. Salois L. Bourgon R. Coulombe S. Mason L. Lamorte C. Sturino R. Bethell Identification and characterization of a novel HIV-1 nucleotide competing RT inhibitor series Antimicrob. Agents Chemother. 2013 57 2712 2718
-
(2013)
Antimicrob. Agents Chemother.
, vol.57
, pp. 2712-2718
-
-
Rajotte, D.1
Tremblay, S.2
Pelletier, A.3
Salois, P.4
Bourgon, L.5
Coulombe, R.6
Mason, S.7
Lamorte, L.8
Sturino, C.9
Bethell, R.10
-
30
-
-
4644270641
-
Novel mechanism of inhibition of HIV-1 reverse transcriptase by a new non-nucleoside analog, KM-1
-
L. Z. Wang G. L. Kenyon K. A. Johnson Novel mechanism of inhibition of HIV-1 reverse transcriptase by a new non-nucleoside analog, KM-1 J. Biol. Chem. 2004 279 38424 38432
-
(2004)
J. Biol. Chem.
, vol.279
, pp. 38424-38432
-
-
Wang, L.Z.1
Kenyon, G.L.2
Johnson, K.A.3
-
31
-
-
0036910799
-
A novel mechanism for inhibition of HIV-1 reverse transcriptase
-
A. G. Skillman K. W. Maurer D. C. Roe M. J. Stauber D. Eargle T. J. Ewing A. Muscate E. Davioud-Charvet M. V. Medaglia R. J. Fisher E. Arnold H. Q. Gao R. Buckheit P. L. Boyer S. H. Hughes I. D. Kuntz G. L. Kenyon A novel mechanism for inhibition of HIV-1 reverse transcriptase Bioorg. Chem. 2002 30 443 458
-
(2002)
Bioorg. Chem.
, vol.30
, pp. 443-458
-
-
Skillman, A.G.1
Maurer, K.W.2
Roe, D.C.3
Stauber, M.J.4
Eargle, D.5
Ewing, T.J.6
Muscate, A.7
Davioud-Charvet, E.8
Medaglia, M.V.9
Fisher, R.J.10
Arnold, E.11
Gao, H.Q.12
Buckheit, R.13
Boyer, P.L.14
Hughes, S.H.15
Kuntz, I.D.16
Kenyon, G.L.17
-
32
-
-
34447574625
-
Aptamer displacement identifies alternative small-molecule target sites that escape viral resistance
-
S. Yamazaki L. Tan G. Mayer J. S. Hartig J. N. Song S. Reuter T. Restle S. D. Laufer D. Grohmann H. G. Kräusslich J. Bajorath M. Famulok Aptamer displacement identifies alternative small-molecule target sites that escape viral resistance Chem. Biol. 2007 14 804 812
-
(2007)
Chem. Biol.
, vol.14
, pp. 804-812
-
-
Yamazaki, S.1
Tan, L.2
Mayer, G.3
Hartig, J.S.4
Song, J.N.5
Reuter, S.6
Restle, T.7
Laufer, S.D.8
Grohmann, D.9
Kräusslich, H.G.10
Bajorath, J.11
Famulok, M.12
-
33
-
-
37849042508
-
Mechanism of inhibition of HIV-1 reverse transcriptase by the novel broad-range DNA polymerase inhibitor N-{2-[4-(aminosulfonyl) phenyl]ethyl}-2-(2-thienyl)acetamide
-
A. Herschhorn I. Oz-Gleenberg A. Hizi Mechanism of inhibition of HIV-1 reverse transcriptase by the novel broad-range DNA polymerase inhibitor N-{2-[4-(aminosulfonyl) phenyl]ethyl}-2-(2-thienyl)acetamide Biochemistry 2008 47 490 502
-
(2008)
Biochemistry
, vol.47
, pp. 490-502
-
-
Herschhorn, A.1
Oz-Gleenberg, I.2
Hizi, A.3
-
34
-
-
57149142659
-
Recent advances in the research of HIV-1 RNase H inhibitors
-
F. Yu X. Liu P. Zhan E. De Clercq Recent advances in the research of HIV-1 RNase H inhibitors Mini-Rev. Med. Chem. 2008 8 1243 1251
-
(2008)
Mini-Rev. Med. Chem.
, vol.8
, pp. 1243-1251
-
-
Yu, F.1
Liu, X.2
Zhan, P.3
De Clercq, E.4
-
35
-
-
84899821420
-
Recent progress in the research of small molecule HIV-1 RNase H inhibitors
-
L. Cao W. Song E. De Clercq P. Zhan X. Liu Recent progress in the research of small molecule HIV-1 RNase H inhibitors Curr. Med. Chem. 2014 21 1956 1967
-
(2014)
Curr. Med. Chem.
, vol.21
, pp. 1956-1967
-
-
Cao, L.1
Song, W.2
De Clercq, E.3
Zhan, P.4
Liu, X.5
-
36
-
-
77955648999
-
HIV-1 RT-associated RNase H function inhibitors: Recent advances in drug development
-
E. Tramontano R. Di Santo HIV-1 RT-associated RNase H function inhibitors: recent advances in drug development Curr. Med. Chem. 2010 17 2837 2853
-
(2010)
Curr. Med. Chem.
, vol.17
, pp. 2837-2853
-
-
Tramontano, E.1
Di Santo, R.2
-
37
-
-
79960189034
-
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H
-
S. Chung D. M. Himmel J. K. Jiang K. Wojtak J. D. Bauman J. W. Rausch J. A. Wilson J. A. Beutler C. J. Thomas E. Arnold S. F. Le Grice Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H J. Med. Chem. 2011 54 4462 4473
-
(2011)
J. Med. Chem.
, vol.54
, pp. 4462-4473
-
-
Chung, S.1
Himmel, D.M.2
Jiang, J.K.3
Wojtak, K.4
Bauman, J.D.5
Rausch, J.W.6
Wilson, J.A.7
Beutler, J.A.8
Thomas, C.J.9
Arnold, E.10
Le Grice, S.F.11
-
38
-
-
20044387576
-
Selective inhibition of HIV-1 reverse transcriptase-associated ribonuclease H activity by hydroxylated tropolones
-
S. R. Budihas I. Gorshkova S. Gaidamakov A. Wamiru M. K. Bona M. A. Parniak R. J. Crouch J. B. McMahon J. A. Beutler S. F. Le Grice Selective inhibition of HIV-1 reverse transcriptase-associated ribonuclease H activity by hydroxylated tropolones Nucleic Acids Res. 2005 33 1249 1256
-
(2005)
Nucleic Acids Res.
, vol.33
, pp. 1249-1256
-
-
Budihas, S.R.1
Gorshkova, I.2
Gaidamakov, S.3
Wamiru, A.4
Bona, M.K.5
Parniak, M.A.6
Crouch, R.J.7
McMahon, J.B.8
Beutler, J.A.9
Le Grice, S.F.10
-
39
-
-
71049185147
-
Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site
-
D. M. Himmel K. A. Maegley T. A. Pauly J. D. Bauman K. Das C. Dharia A. D. Clark Jr. K. Ryan M. J. Hickey R. A. Love S. H. Hughes S. Bergqvist E. Arnold Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site Structure 2009 17 1625 1635
-
(2009)
Structure
, vol.17
, pp. 1625-1635
-
-
Himmel, D.M.1
Maegley, K.A.2
Pauly, T.A.3
Bauman, J.D.4
Das, K.5
Dharia, C.6
Clark, Jr.A.D.7
Ryan, K.8
Hickey, M.J.9
Love, R.A.10
Hughes, S.H.11
Bergqvist, S.12
Arnold, E.13
-
40
-
-
11144355815
-
Activity of the isolated HIV RNase H domain and specific inhibition by N-hydroxyimides
-
J. Q. Hang S. Rajendran Y. Yang Y. Li P. W. In H. Overton K. E. Parkes N. Cammack J. A. Martin K. Klumpp Activity of the isolated HIV RNase H domain and specific inhibition by N-hydroxyimides Biochem. Biophys. Res. Commun. 2004 317 321 329
-
(2004)
Biochem. Biophys. Res. Commun.
, vol.317
, pp. 321-329
-
-
Hang, J.Q.1
Rajendran, S.2
Yang, Y.3
Li, Y.4
In, P.W.5
Overton, H.6
Parkes, K.E.7
Cammack, N.8
Martin, J.A.9
Klumpp, K.10
-
41
-
-
84861572493
-
Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity
-
V. Suchaud F. Bailly C. Lion E. Tramontano F. Esposito A. Corona F. Christ Z. Debyser P. Cotelle Development of a series of 3-hydroxyquinolin-2(1H)- ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity Bioorg. Med. Chem. Lett. 2012 22 3988 3992
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 3988-3992
-
-
Suchaud, V.1
Bailly, F.2
Lion, C.3
Tramontano, E.4
Esposito, F.5
Corona, A.6
Christ, F.7
Debyser, Z.8
Cotelle, P.9
-
42
-
-
79952789620
-
Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: Discovery of a novel selective inhibitor of the ribonuclease H function
-
M. Billamboz F. Bailly C. Lion N. Touati H. Vezin C. Calmels M. L. Andréola F. Christ Z. Debyser P. Cotelle Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function J. Med. Chem. 2011 54 1812 1824
-
(2011)
J. Med. Chem.
, vol.54
, pp. 1812-1824
-
-
Billamboz, M.1
Bailly, F.2
Lion, C.3
Touati, N.4
Vezin, H.5
Calmels, C.6
Andréola, M.L.7
Christ, F.8
Debyser, Z.9
Cotelle, P.10
-
43
-
-
70349638920
-
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: Design, biochemical activity, and structural information
-
T. A. Kirschberg M. Balakrishnan N. H. Squires T. Barnes K. M. Brendza X. Chen E. J. Eisenberg W. Jin N. Kutty S. Leavitt A. Liclican Q. Liu X. Liu J. Mak J. K. Perry M. Wang W. J. Watkins E. B. Lansdon RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information J. Med. Chem. 2009 52 5781 5784
-
(2009)
J. Med. Chem.
, vol.52
, pp. 5781-5784
-
-
Kirschberg, T.A.1
Balakrishnan, M.2
Squires, N.H.3
Barnes, T.4
Brendza, K.M.5
Chen, X.6
Eisenberg, E.J.7
Jin, W.8
Kutty, N.9
Leavitt, S.10
Liclican, A.11
Liu, Q.12
Liu, X.13
Mak, J.14
Perry, J.K.15
Wang, M.16
Watkins, W.J.17
Lansdon, E.B.18
-
44
-
-
79956334444
-
Structural and binding analysis of pyrimidinol carboxylic acid and N-hydroxy quinazolinedione HIV-1 RNase H inhibitors
-
E. B. Lansdon Q. Liu S. A. Leavitt M. Balakrishnan J. K. Perry C. Lancaster-Moyer N. Kutty X. Liu N. H. Squires W. J. Watkins T. A. Kirschberg Structural and binding analysis of pyrimidinol carboxylic acid and N-hydroxy quinazolinedione HIV-1 RNase H inhibitors Antimicrob. Agents Chemother. 2011 55 2905 2915
-
(2011)
Antimicrob. Agents Chemother.
, vol.55
, pp. 2905-2915
-
-
Lansdon, E.B.1
Liu, Q.2
Leavitt, S.A.3
Balakrishnan, M.4
Perry, J.K.5
Lancaster-Moyer, C.6
Kutty, N.7
Liu, X.8
Squires, N.H.9
Watkins, W.J.10
Kirschberg, T.A.11
-
45
-
-
13544276913
-
6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitro
-
E. Tramontano F. Esposito R. Badas R. Di Santo R. Costi P. La Colla 6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitro Antiviral Res. 2005 65 117 124
-
(2005)
Antiviral Res.
, vol.65
, pp. 117-124
-
-
Tramontano, E.1
Esposito, F.2
Badas, R.3
Di Santo, R.4
Costi, R.5
La Colla, P.6
-
46
-
-
0037474193
-
Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid
-
C. A. Shaw-Reid V. Munshi P. Graham A. Wolfe M. Witmer R. Danzeisen D. B. Olsen S. S. Carroll M. Embrey J. S. Wai M. D. Miller J. L. Cole D. J. Hazuda Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino) thien-2-yl]-2,4-dioxobutanoic acid J. Biol. Chem. 2003 278 2777 2780
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 2777-2780
-
-
Shaw-Reid, C.A.1
Munshi, V.2
Graham, P.3
Wolfe, A.4
Witmer, M.5
Danzeisen, R.6
Olsen, D.B.7
Carroll, S.S.8
Embrey, M.9
Wai, J.S.10
Miller, M.D.11
Cole, J.L.12
Hazuda, D.J.13
-
47
-
-
77954521861
-
Structural basis for the inhibition of RNaseH activity of HIV-1 Reverse Transcriptase by RNaseH active site-directed inhibitors
-
H. P. Su Y. Yan G. S. Prasad R. F. Smith C. L. Daniels P. D. Abeywickrema J. C. Reid H. M. Loughran M. Kornienko S. Sharma J. A. Grobler B. Xu V. Sardana T. J. Allison P. D. Williams P. L. Darke D. J. Hazuda S. Munshi Structural basis for the inhibition of RNaseH activity of HIV-1 Reverse Transcriptase by RNaseH active site-directed inhibitors J. Virol. 2010 84 7625 7633
-
(2010)
J. Virol.
, vol.84
, pp. 7625-7633
-
-
Su, H.P.1
Yan, Y.2
Prasad, G.S.3
Smith, R.F.4
Daniels, C.L.5
Abeywickrema, P.D.6
Reid, J.C.7
Loughran, H.M.8
Kornienko, M.9
Sharma, S.10
Grobler, J.A.11
Xu, B.12
Sardana, V.13
Allison, T.J.14
Williams, P.D.15
Darke, P.L.16
Hazuda, D.J.17
Munshi, S.18
-
48
-
-
77958045051
-
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold
-
P. D. Williams D. D. Staas S. Venkatraman H. M. Loughran R. D. Ruzek T. M. Booth T. A. Lyle J. S. Wai J. P. Vacca B. P. Feuston L. T. Ecto J. A. Flynn D. J. Distefano D. J. Hazuda C. M. Bahnck A. L. Himmelberger G. Dornadula R. C. Hrin K. A. Stillmock M. V. Witmer M. D. Miller J. A. Grobler Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin- 2(1H)-one scaffold Bioorg. Med. Chem. Lett. 2010 20 6754 6757
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 6754-6757
-
-
Williams, P.D.1
Staas, D.D.2
Venkatraman, S.3
Loughran, H.M.4
Ruzek, R.D.5
Booth, T.M.6
Lyle, T.A.7
Wai, J.S.8
Vacca, J.P.9
Feuston, B.P.10
Ecto, L.T.11
Flynn, J.A.12
Distefano, D.J.13
Hazuda, D.J.14
Bahnck, C.M.15
Himmelberger, A.L.16
Dornadula, G.17
Hrin, R.C.18
Stillmock, K.A.19
Witmer, M.V.20
Miller, M.D.21
Grobler, J.A.22
more..
-
49
-
-
84863338007
-
Structural and inhibition studies of the RNase H function of xenotropic murine leukemia virus-related virus reverse transcriptase
-
K. A. Kirby B. Marchand Y. T. Ong T. P. Ndongwe A. Hachiya E. Michailidis M. D. Leslie D. V. Sietsema T. L. Fetterly C. A. Dorst K. Singh Z. Wang M. A. Parniak S. G. Sarafianos Structural and inhibition studies of the RNase H function of xenotropic murine leukemia virus-related virus reverse transcriptase Antimicrob. Agents Chemother. 2012 56 2048 2061
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 2048-2061
-
-
Kirby, K.A.1
Marchand, B.2
Ong, Y.T.3
Ndongwe, T.P.4
Hachiya, A.5
Michailidis, E.6
Leslie, M.D.7
Sietsema, D.V.8
Fetterly, T.L.9
Dorst, C.A.10
Singh, K.11
Wang, Z.12
Parniak, M.A.13
Sarafianos, S.G.14
-
50
-
-
78651513267
-
Structural and biochemical study on the inhibitory activity of derivatives of 5-nitro-furan-2-carboxylic acid for RNase H function of HIV-1 reverse transcriptase
-
H. Yanagita E. Urano K. Matsumoto R. Ichikawa Y. Takaesu M. Ogata T. Murakami H. Wu J. Chiba J. Komano T. Hoshino Structural and biochemical study on the inhibitory activity of derivatives of 5-nitro-furan-2-carboxylic acid for RNase H function of HIV-1 reverse transcriptase Bioorg. Med. Chem. 2011 19 816 825
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 816-825
-
-
Yanagita, H.1
Urano, E.2
Matsumoto, K.3
Ichikawa, R.4
Takaesu, Y.5
Ogata, M.6
Murakami, T.7
Wu, H.8
Chiba, J.9
Komano, J.10
Hoshino, T.11
-
51
-
-
64349084459
-
Derivatives of 5-nitro-furan-2-carboxylic acid carbamoylmethyl ester inhibit RNase H activity associated with HIV-1 reverse transcriptase
-
H. Fuji E. Urano Y. Futahashi M. Hamatake J. Tatsumi T. Hoshino Y. Morikawa N. Yamamoto J. Komano Derivatives of 5-nitro-furan-2-carboxylic acid carbamoylmethyl ester inhibit RNase H activity associated with HIV-1 reverse transcriptase J. Med. Chem. 2009 52 1380 1387
-
(2009)
J. Med. Chem.
, vol.52
, pp. 1380-1387
-
-
Fuji, H.1
Urano, E.2
Futahashi, Y.3
Hamatake, M.4
Tatsumi, J.5
Hoshino, T.6
Morikawa, Y.7
Yamamoto, N.8
Komano, J.9
-
52
-
-
58149160464
-
Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity
-
M. Wendeler H. F. Lee A. Bermingham J. T. Miller O. Chertov M. K. Bona N. S. Baichoo M. Ehteshami J. Beutler B. R. O'Keefe M. Götte M. L. Kvaratskhelia S. Grice Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity ACS Chem. Biol. 2008 3 635 644
-
(2008)
ACS Chem. Biol.
, vol.3
, pp. 635-644
-
-
Wendeler, M.1
Lee, H.F.2
Bermingham, A.3
Miller, J.T.4
Chertov, O.5
Bona, M.K.6
Baichoo, N.S.7
Ehteshami, M.8
Beutler, J.9
O'Keefe, B.R.10
Götte, M.11
Kvaratskhelia, M.L.12
Grice, S.13
-
53
-
-
84880165792
-
Exploiting Drug-Resistant Enzymes as Tools to Identify Thienopyrimidinone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H
-
T. Masaoka S. Chung P. Caboni J. Rausch J. A. Wilson H. Taskent-Sezgin J. A. Beutler G. L. Tocco S. F. Grice Exploiting Drug-Resistant Enzymes as Tools to Identify Thienopyrimidinone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H J. Med. Chem. 2013 56 5436 5445
-
(2013)
J. Med. Chem.
, vol.56
, pp. 5436-5445
-
-
Masaoka, T.1
Chung, S.2
Caboni, P.3
Rausch, J.4
Wilson, J.A.5
Taskent-Sezgin, H.6
Beutler, J.A.7
Tocco, G.L.8
Grice, S.F.9
-
54
-
-
37249062449
-
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site
-
D. M. Himmel S. G. Sarafianos S. Dharmasena M. M. Hossain K. McCoy-Simandle T. Ilina A. D. Clark Jr. J. L. Knight J. G. Julias P. K. Clark K. Krogh-Jespersen R. M. Levy S. H. Hughes M. A. Parniak E. Arnold HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site ACS Chem. Biol. 2006 1 702 712
-
(2006)
ACS Chem. Biol.
, vol.1
, pp. 702-712
-
-
Himmel, D.M.1
Sarafianos, S.G.2
Dharmasena, S.3
Hossain, M.M.4
McCoy-Simandle, K.5
Ilina, T.6
Clark, Jr.A.D.7
Knight, J.L.8
Julias, J.G.9
Clark, P.K.10
Krogh-Jespersen, K.11
Levy, R.M.12
Hughes, S.H.13
Parniak, M.A.14
Arnold, E.15
-
55
-
-
80051975966
-
Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studies
-
A. K. Felts K. Labarge J. D. Bauman D. V. Patel D. M. Himmel E. Arnold M. A. Parniak R. M. Levy Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studies J. Chem. Inf. Model. 2011 51 1986 1998
-
(2011)
J. Chem. Inf. Model.
, vol.51
, pp. 1986-1998
-
-
Felts, A.K.1
Labarge, K.2
Bauman, J.D.3
Patel, D.V.4
Himmel, D.M.5
Arnold, E.6
Parniak, M.A.7
Levy, R.M.8
-
57
-
-
79955072485
-
Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases
-
F. Esposito T. Kharlamova S. Distinto L. Zinzula Y. C. Cheng G. Dutschman G. Floris P. Markt A. Corona E. Tramontano Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases FEBS J. 2011 278 1444 1457
-
(2011)
FEBS J.
, vol.278
, pp. 1444-1457
-
-
Esposito, F.1
Kharlamova, T.2
Distinto, S.3
Zinzula, L.4
Cheng, Y.C.5
Dutschman, G.6
Floris, G.7
Markt, P.8
Corona, A.9
Tramontano, E.10
-
58
-
-
84858440068
-
Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D fingerprint- and pharmacophore-based virtual screening approach
-
S. Distinto F. Esposito J. Kirchmair M. C. Cardia M. Gaspari E. Maccioni S. Alcaro P. Markt G. Wolber L. Zinzula E. Tramontano Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D fingerprint- and pharmacophore-based virtual screening approach Eur. J. Med. Chem. 2012 50 216 229
-
(2012)
Eur. J. Med. Chem.
, vol.50
, pp. 216-229
-
-
Distinto, S.1
Esposito, F.2
Kirchmair, J.3
Cardia, M.C.4
Gaspari, M.5
Maccioni, E.6
Alcaro, S.7
Markt, P.8
Wolber, G.9
Zinzula, L.10
Tramontano, E.11
-
59
-
-
0242502660
-
HIV-1 reverse transcription: A brief overview focused on structure-function relationships among molecules involved in the initiation of the reaction
-
M. Gotte X. Li M. A. Wainberg HIV-1 reverse transcription: A brief overview focused on structure-function relationships among molecules involved in the initiation of the reaction Arch. Biochem. Biophys. 1999 365 199 210
-
(1999)
Arch. Biochem. Biophys.
, vol.365
, pp. 199-210
-
-
Gotte, M.1
Li, X.2
Wainberg, M.A.3
-
60
-
-
0037166260
-
Primer unblocking and rescue of DNA synthesis by azidothymidine (AZT)-resistant HIV-1 reverse transcriptase
-
M. Rigourd C. Ehresmann M. A. Parniak B. Ehresmann R. Marquet Primer unblocking and rescue of DNA synthesis by azidothymidine (AZT)-resistant HIV-1 reverse transcriptase J. Biol. Chem. 2002 277 18611 18618
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 18611-18618
-
-
Rigourd, M.1
Ehresmann, C.2
Parniak, M.A.3
Ehresmann, B.4
Marquet, R.5
-
61
-
-
84876221270
-
Detecting Allosteric Sites of HIV-1 Reverse Transcriptase by X-ray Crystallographic Fragment Screening
-
J. D. Bauman D. Patel C. Dharia M. W. Fromer S. Ahmed Y. Frenkel R. S. Vijayan J. T. Eck W. C. Ho K. Das A. J. Shatkin E. Arnold Detecting Allosteric Sites of HIV-1 Reverse Transcriptase by X-ray Crystallographic Fragment Screening J. Med. Chem. 2013 56 2738 2746
-
(2013)
J. Med. Chem.
, vol.56
, pp. 2738-2746
-
-
Bauman, J.D.1
Patel, D.2
Dharia, C.3
Fromer, M.W.4
Ahmed, S.5
Frenkel, Y.6
Vijayan, R.S.7
Eck, J.T.8
Ho, W.C.9
Das, K.10
Shatkin, A.J.11
Arnold, E.12
-
62
-
-
80052987412
-
Recent developments of peptidomimetic HIV-1 protease inhibitors
-
X. Qiu Z. P. Liu Recent developments of peptidomimetic HIV-1 protease inhibitors Curr. Med. Chem. 2011 18 4513 4537
-
(2011)
Curr. Med. Chem.
, vol.18
, pp. 4513-4537
-
-
Qiu, X.1
Liu, Z.P.2
-
63
-
-
27344455412
-
From nonpeptide toward noncarbon protease inhibitors: Metallacarboranes as specific and potent inhibitors of HIV protease
-
P. Cígler M. Kozísek P. Rezácová J. Brynda Z. Otwinowski J. Pokorná J. Plesek B. Grüner L. Dolecková- Maresová M. Mása J. Sedlácek J. Bodem H. G. Kräusslich V. Král J. Konvalinka From nonpeptide toward noncarbon protease inhibitors: metallacarboranes as specific and potent inhibitors of HIV protease Proc. Natl. Acad. Sci. U. S. A. 2005 102 15394 15399
-
(2005)
Proc. Natl. Acad. Sci. U. S. A.
, vol.102
, pp. 15394-15399
-
-
Cígler, P.1
Kozísek, M.2
Rezácová, P.3
Brynda, J.4
Otwinowski, Z.5
Pokorná, J.6
Plesek, J.7
Grüner, B.8
Dolecková- Maresová, L.9
Mása, M.10
Sedlácek, J.11
Bodem, J.12
Kräusslich, H.G.13
Král, V.14
Konvalinka, J.15
-
64
-
-
49449113806
-
Inorganic polyhedral metallacarborane inhibitors of HIV protease: A new approach to overcoming antiviral resistance
-
M. Kozísek P. Cígler M. Lepsík J. Fanfrlík P. Rezácová J. Brynda J. Pokorná J. Plesek B. Grüner S. K. Grantz J. Václavíková V. Král J. Konvalinka Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance J. Med. Chem. 2008 51 4839 4843
-
(2008)
J. Med. Chem.
, vol.51
, pp. 4839-4843
-
-
Kozísek, M.1
Cígler, P.2
Lepsík, M.3
Fanfrlík, J.4
Rezácová, P.5
Brynda, J.6
Pokorná, J.7
Plesek, J.8
Grüner, B.9
Grantz, S.K.10
Václavíková, J.11
Král, V.12
Konvalinka, J.13
-
65
-
-
71049176193
-
Design of HIV protease inhibitors based on inorganic polyhedral metallacarboranes
-
P. Rezácová J. Pokorná J. Brynda M. Kozísek P. Cígler M. Lepsík J. Fanfrlík J. Rezác K. Grantz-Sasková I. Sieglová J. Plesek V. Sícha B. Grüner H. Oberwinkler J. Sedlácek' H. G. Kräusslich P. Hobza V. Král J. Konvalinka Design of HIV protease inhibitors based on inorganic polyhedral metallacarboranes J. Med. Chem. 2009 52 7132 7141
-
(2009)
J. Med. Chem.
, vol.52
, pp. 7132-7141
-
-
Rezácová, P.1
Pokorná, J.2
Brynda, J.3
Kozísek, M.4
Cígler, P.5
Lepsík, M.6
Fanfrlík, J.7
Rezác, J.8
Grantz-Sasková, K.9
Sieglová, I.10
Plesek, J.11
Sícha, V.12
Grüner, B.13
Oberwinkler, H.14
Sedlácek'J15
Kräusslich, H.G.16
Hobza, P.17
Král, V.18
Konvalinka, J.19
-
66
-
-
84870027189
-
Structure-aided design of novel inhibitors of HIV protease based on a benzodiazepine scaffold
-
J. Schimer P. Cígler J. Veselý K. Grantz- ŠaŠková M. LepŠík J. Brynda P. Rezáčová M. KožíŠek I. Císařová H. Oberwinkler H. G. Kraeusslich J. Konvalinka Structure-aided design of novel inhibitors of HIV protease based on a benzodiazepine scaffold J. Med. Chem. 2012 55 10130 10135
-
(2012)
J. Med. Chem.
, vol.55
, pp. 10130-10135
-
-
Schimer, J.1
Cígler, P.2
Veselý, J.3
Grantz- Šašková, K.4
Lepšík, M.5
Brynda, J.6
Rezáčová, P.7
Kožíšek, M.8
Císařová, I.9
Oberwinkler, H.10
Kraeusslich, H.G.11
Konvalinka, J.12
-
67
-
-
84879761645
-
Small Molecule Regulation of Protein Conformation by Binding in the Flap of HIV Protease
-
T. Tiefenbrunn S. Forli M. M. Baksh M. W. Chang M. Happer Y. C. Lin A. L. Perryman J. K. Rhee B. E. Torbett A. J. Olson J. H. Elder M. G. Finn C. D. Stout Small Molecule Regulation of Protein Conformation by Binding in the Flap of HIV Protease ACS Chem. Biol. 2013 8 1223 1231
-
(2013)
ACS Chem. Biol.
, vol.8
, pp. 1223-1231
-
-
Tiefenbrunn, T.1
Forli, S.2
Baksh, M.M.3
Chang, M.W.4
Happer, M.5
Lin, Y.C.6
Perryman, A.L.7
Rhee, J.K.8
Torbett, B.E.9
Olson, A.J.10
Elder, J.H.11
Finn, M.G.12
Stout, C.D.13
-
68
-
-
77957931762
-
Targeting protein-protein interactions: A promising avenue of anti-HIV drug discovery
-
P. Zhan W. Li H. Chen X. Liu Targeting protein-protein interactions: a promising avenue of anti-HIV drug discovery Curr. Med. Chem. 2010 17 3393 3409
-
(2010)
Curr. Med. Chem.
, vol.17
, pp. 3393-3409
-
-
Zhan, P.1
Li, W.2
Chen, H.3
Liu, X.4
-
69
-
-
84864957267
-
Carbonylhydrazide-based molecular tongs inhibit wild-type and mutated HIV-1 protease dimerization
-
L. Dufau A. S. Marques-Ressurreição R. Fanelli N. Kihal A. Vidu T. Milcent J. L. Soulier-Rodrigo J. De-Losada A. Desvergne K. Leblanc G. Bernadat B. Crousse M. Reboud-Ravaux S. Ongeri Carbonylhydrazide-based molecular tongs inhibit wild-type and mutated HIV-1 protease dimerization J. Med. Chem. 2012 55 6762 6775
-
(2012)
J. Med. Chem.
, vol.55
, pp. 6762-6775
-
-
Dufau, L.1
Marques-Ressurreição, A.S.2
Fanelli, R.3
Kihal, N.4
Vidu, A.5
Milcent, T.6
Soulier-Rodrigo, J.L.7
De-Losada, J.8
Desvergne, A.9
Leblanc, K.10
Bernadat, G.11
Crousse, B.12
Reboud-Ravaux, M.13
Ongeri, S.14
-
70
-
-
84868035469
-
Alkyl hydroxybenzoic acid derivatives that inhibit HIV-1 protease dimerization
-
O. A. Flausino Jr. L. Dufau L. O. Regasini M. S. Petrônio D. H. Silva T. Rose V. S. Bolzani M. Reboud-Ravaux Alkyl hydroxybenzoic acid derivatives that inhibit HIV-1 protease dimerization Curr. Med. Chem. 2012 19 4534 4540
-
(2012)
Curr. Med. Chem.
, vol.19
, pp. 4534-4540
-
-
Flausino, Jr.O.A.1
Dufau, L.2
Regasini, L.O.3
Petrônio, M.S.4
Silva, D.H.5
Rose, T.6
Bolzani, V.S.7
Reboud-Ravaux, M.8
-
71
-
-
84859641222
-
Novel therapeutic strategies targeting HIV integrase
-
P. K. Quashie R. D. Sloan M. A. Wainberg Novel therapeutic strategies targeting HIV integrase BMC Med. 2012 10 34
-
(2012)
BMC Med.
, vol.10
, pp. 34
-
-
Quashie, P.K.1
Sloan, R.D.2
Wainberg, M.A.3
-
72
-
-
84875545671
-
Non-enzymatic functions of retroviral integrase: The next target for novel anti-HIV drug development
-
T. Masuda Non-enzymatic functions of retroviral integrase: the next target for novel anti-HIV drug development Front. Microbiol. 2011 2 210
-
(2011)
Front. Microbiol.
, vol.2
, pp. 210
-
-
Masuda, T.1
-
74
-
-
79251545504
-
Allosteric inhibitor development targeting HIV-1 integrase
-
L. Q. Al-Mawsawi N. Neamati Allosteric inhibitor development targeting HIV-1 integrase ChemMedChem 2011 6 228 241
-
(2011)
ChemMedChem
, vol.6
, pp. 228-241
-
-
Al-Mawsawi, L.Q.1
Neamati, N.2
-
75
-
-
62249176335
-
New approaches for inhibiting HIV integrase: A journey beyond the active site
-
M. A. Walker New approaches for inhibiting HIV integrase: a journey beyond the active site Curr. Opin. Invest. Drugs (BioMed Cent.) 2009 10 129 136
-
(2009)
Curr. Opin. Invest. Drugs (BioMed Cent.)
, vol.10
, pp. 129-136
-
-
Walker, M.A.1
-
76
-
-
50149096422
-
D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75
-
L. Du Y. Zhao J. Chen L. Yang Y. Zheng Y. Tang X. Shen H. Jiang D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75 Biochem. Biophys. Res. Commun. 2008 375 139 144
-
(2008)
Biochem. Biophys. Res. Commun.
, vol.375
, pp. 139-144
-
-
Du, L.1
Zhao, Y.2
Chen, J.3
Yang, L.4
Zheng, Y.5
Tang, Y.6
Shen, X.7
Jiang, H.8
-
77
-
-
77952553431
-
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication
-
F. Christ A. Voet A. Marchand S. Nicolet B. A. Desimmie D. Marchand D. Bardiot N. J. Vander Veken B. Van Remoortel S. V. Strelkov M. De Maeyer P. Chaltin Z. Debyser Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication Nat. Chem. Biol. 2010 6 442 448
-
(2010)
Nat. Chem. Biol.
, vol.6
, pp. 442-448
-
-
Christ, F.1
Voet, A.2
Marchand, A.3
Nicolet, S.4
Desimmie, B.A.5
Marchand, D.6
Bardiot, D.7
Vander Veken, N.J.8
Van Remoortel, B.9
Strelkov, S.V.10
De Maeyer, M.11
Chaltin, P.12
Debyser, Z.13
-
78
-
-
84860871902
-
Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors
-
J. J. Kessl N. Jena Y. Koh H. Taskent-Sezgin A. Slaughter L. Feng S. de Silva L. Wu S. F. Le Grice A. Engelman J. R. Fuchs M. Kvaratskhelia Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors J. Biol. Chem. 2012 287 16801 16811
-
(2012)
J. Biol. Chem.
, vol.287
, pp. 16801-16811
-
-
Kessl, J.J.1
Jena, N.2
Koh, Y.3
Taskent-Sezgin, H.4
Slaughter, A.5
Feng, L.6
De Silva, S.7
Wu, L.8
Le Grice, S.F.9
Engelman, A.10
Fuchs, J.R.11
Kvaratskhelia, M.12
-
79
-
-
84878137599
-
Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation
-
K. A. Jurado H. Wang A. Slaughter L. Feng J. J. Kessl Y. Koh W. Wang A. Ballandras-Colas P. A. Patel J. R. Fuchs M. Kvaratskhelia A. Engelman Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation Proc. Natl. Acad. Sci. U. S. A. 2013 110 8690 8695
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 8690-8695
-
-
Jurado, K.A.1
Wang, H.2
Slaughter, A.3
Feng, L.4
Kessl, J.J.5
Koh, Y.6
Wang, W.7
Ballandras-Colas, A.8
Patel, P.A.9
Fuchs, J.R.10
Kvaratskhelia, M.11
Engelman, A.12
-
80
-
-
84903765176
-
-
BI 224436, a non-catalytic site integrase inhibitor, is a potent inhibitor of the replication of treatment-naïve and raltegravir-resistant clinical isolates of HIV-1. In 51st Interscience Conference on Antimicrobials and Chemotherapy: 2011; Chicago, IL, USA; 2011. Levin: Conference Reports for NATAP; 2011
-
C. Fenwick, R. Bethell, M. Cordingley, P. Edwards, A.-M. Quinson, P. Robinson, B. Simoneau and C. Yoakim, BI 224436, a non-catalytic site integrase inhibitor, is a potent inhibitor of the replication of treatment-naïve and raltegravir-resistant clinical isolates of HIV-1. In 51st Interscience Conference on Antimicrobials and Chemotherapy: 2011; Chicago, IL, USA; 2011. Levin: Conference Reports for NATAP; 2011, http://www.natap.org/2011/ICAAC/ ICAAC-34.htm
-
-
-
Fenwick, C.1
Bethell, R.2
Cordingley, M.3
Edwards, P.4
Quinson, A.-M.5
Robinson, P.6
Simoneau, B.7
Yoakim, C.8
-
81
-
-
84903752550
-
-
Safety and pharmacokinetics (PK) of single rising oral doses of a novel HIV integrase inhibitor in healthy volunteers. In 51st Interscience Conference on Antimicrobials and Chemotherapy: 2011; Chicago, IL, USA; 2011. Levin: Conference Reports for NATAP; 2011
-
S. Aslanyan, C. H. Ballow, J. P. Sabo, J. Habeck, D. Roos, T. R. MacGregor, P. Robinson and J. Kort, Safety and pharmacokinetics (PK) of single rising oral doses of a novel HIV integrase inhibitor in healthy volunteers. In 51st Interscience Conference on Antimicrobials and Chemotherapy: 2011; Chicago, IL, USA; 2011. Levin: Conference Reports for NATAP; 2011, http://www.natap.org/ 2011/ICAAC/ICAAC-35.htm
-
-
-
Aslanyan, S.1
Ballow, C.H.2
Sabo, J.P.3
Habeck, J.4
Roos, D.5
Macgregor, T.R.6
Robinson, P.7
Kort, J.8
-
82
-
-
84864387134
-
Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization
-
F. Christ S. Shaw J. Demeulemeester B. A. Desimmie A. Marchand S. Butler W. Smets P. Chaltin M. Westby Z. Debyser C. Pickford Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization Antimicrob. Agents Chemother. 2012 56 4365 4374
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 4365-4374
-
-
Christ, F.1
Shaw, S.2
Demeulemeester, J.3
Desimmie, B.A.4
Marchand, A.5
Butler, S.6
Smets, W.7
Chaltin, P.8
Westby, M.9
Debyser, Z.10
Pickford, C.11
-
83
-
-
84862271587
-
New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action
-
M. Tsiang G. S. Jones A. Niedziela-Majka E. Kan E. B. Lansdon W. Huang M. Hung D. Samuel N. Novikov Y. Xu M. Mitchell H. Guo K. Babaoglu X. Liu R. Geleziunas R. Sakowicz New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action J. Biol. Chem. 2012 287 21189 21203
-
(2012)
J. Biol. Chem.
, vol.287
, pp. 21189-21203
-
-
Tsiang, M.1
Jones, G.S.2
Niedziela-Majka, A.3
Kan, E.4
Lansdon, E.B.5
Huang, W.6
Hung, M.7
Samuel, D.8
Novikov, N.9
Xu, Y.10
Mitchell, M.11
Guo, H.12
Babaoglu, K.13
Liu, X.14
Geleziunas, R.15
Sakowicz, R.16
-
84
-
-
84903770581
-
-
WO2012033735 A1
-
P. Annapurna, L. Guo, G. Samuel, R. L. David, L. T. George and M. Nicholas, Inhibitors of human immunodeficiency virus replication, WO2012033735 A1, 2012
-
(2012)
Inhibitors of Human Immunodeficiency Virus Replication
-
-
Annapurna, P.1
Guo, L.2
Samuel, G.3
David, R.L.4
George, L.T.5
Nicholas, M.6
-
85
-
-
68149149956
-
Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75
-
L. De Luca M. L. Barreca S. Ferro F. Christ N. Iraci R. Gitto A. M. Monforte Z. Debyser A. Chimirri Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75 ChemMedChem 2009 4 1311 1316
-
(2009)
ChemMedChem
, vol.4
, pp. 1311-1316
-
-
De Luca, L.1
Barreca, M.L.2
Ferro, S.3
Christ, F.4
Iraci, N.5
Gitto, R.6
Monforte, A.M.7
Debyser, Z.8
Chimirri, A.9
-
86
-
-
77958015795
-
Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor
-
L. De Luca S. Ferro R. Gitto M. L. Barreca S. Agnello F. Christ Z. Debyser A. Chimirri Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor Bioorg. Med. Chem. 2010 18 7515 7521
-
(2010)
Bioorg. Med. Chem.
, vol.18
, pp. 7515-7521
-
-
De Luca, L.1
Ferro, S.2
Gitto, R.3
Barreca, M.L.4
Agnello, S.5
Christ, F.6
Debyser, Z.7
Chimirri, A.8
-
87
-
-
80052862237
-
4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process
-
L. De Luca R. Gitto F. Christ S. Ferro S. De Grazia F. Morreale Z. Debyser A. Chimirri 4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4- oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process Antiviral Res. 2011 92 102 107
-
(2011)
Antiviral Res.
, vol.92
, pp. 102-107
-
-
De Luca, L.1
Gitto, R.2
Christ, F.3
Ferro, S.4
De Grazia, S.5
Morreale, F.6
Debyser, Z.7
Chimirri, A.8
-
88
-
-
79961170232
-
Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: A scaffold hopping approach using salicylate and catechol groups
-
X. Fan F. H. Zhang R. I. Al-Safi L. F. Zeng Y. Shabaik B. Debnath T. W. Sanchez S. Odde N. Neamati Y. Q. Long Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: A scaffold hopping approach using salicylate and catechol groups Bioorg. Med. Chem. 2011 19 4935 4952
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 4935-4952
-
-
Fan, X.1
Zhang, F.H.2
Al-Safi, R.I.3
Zeng, L.F.4
Shabaik, Y.5
Debnath, B.6
Sanchez, T.W.7
Odde, S.8
Neamati, N.9
Long, Y.Q.10
-
89
-
-
84869988552
-
Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays
-
G. Hu X. Li X. Zhang Y. Li L. Ma L. M. Yang G. Liu W. Li J. Huang X. Shen L. Hu Y. T. Zheng Y. Tang Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays J. Med. Chem. 2012 55 10108 10117
-
(2012)
J. Med. Chem.
, vol.55
, pp. 10108-10117
-
-
Hu, G.1
Li, X.2
Zhang, X.3
Li, Y.4
Ma, L.5
Yang, L.M.6
Liu, G.7
Li, W.8
Huang, J.9
Shen, X.10
Hu, L.11
Zheng, Y.T.12
Tang, Y.13
-
91
-
-
84875759707
-
Fragment-Based Discovery of 8-Hydroxyquinoline Inhibitors of the HIV-1 Integrase-Lens Epithelium-Derived Growth Factor/p75 (IN-LEDGF/p75) Interaction
-
E. Serrao B. Debnath H. Otake Y. Kuang F. Christ Z. Debyser N. Neamati Fragment-Based Discovery of 8-Hydroxyquinoline Inhibitors of the HIV-1 Integrase-Lens Epithelium-Derived Growth Factor/p75 (IN-LEDGF/p75) Interaction J. Med. Chem. 2013 56 2311 2322
-
(2013)
J. Med. Chem.
, vol.56
, pp. 2311-2322
-
-
Serrao, E.1
Debnath, B.2
Otake, H.3
Kuang, Y.4
Christ, F.5
Debyser, Z.6
Neamati, N.7
-
92
-
-
79952588405
-
LEDGF dominant interference proteins demonstrate prenuclear exposure of HIV-1 integrase and synergize with LEDGF depletion to destroy viral infectivity
-
A. M. Meehan D. T. Saenz J. Morrison C. Hu M. Peretz E. M. Poeschla LEDGF dominant interference proteins demonstrate prenuclear exposure of HIV-1 integrase and synergize with LEDGF depletion to destroy viral infectivity J. Virol. 2011 85 3570 3583
-
(2011)
J. Virol.
, vol.85
, pp. 3570-3583
-
-
Meehan, A.M.1
Saenz, D.T.2
Morrison, J.3
Hu, C.4
Peretz, M.5
Poeschla, E.M.6
-
93
-
-
84869081642
-
Phage Display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication
-
B. A. Desimmie M. Humbert E. Lescrinier J. Hendrix S. Vets R. Gijsbers R. M. Ruprecht U. Dietrich Z. Debyser F. Christ Phage Display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication Mol. Ther. 2012 20 2064 2075
-
(2012)
Mol. Ther.
, vol.20
, pp. 2064-2075
-
-
Desimmie, B.A.1
Humbert, M.2
Lescrinier, E.3
Hendrix, J.4
Vets, S.5
Gijsbers, R.6
Ruprecht, R.M.7
Dietrich, U.8
Debyser, Z.9
Christ, F.10
-
94
-
-
84880179036
-
Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors
-
Y. Q. Long S. X. Huang Z. Zawahir Z. L. Xu H. Li T. W. Sanchez Y. Zhi S. De Houwer F. Christ Z. Debyser N. Neamati Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors J. Med. Chem. 2013 56 5601 5612
-
(2013)
J. Med. Chem.
, vol.56
, pp. 5601-5612
-
-
Long, Y.Q.1
Huang, S.X.2
Zawahir, Z.3
Xu, Z.L.4
Li, H.5
Sanchez, T.W.6
Zhi, Y.7
De Houwer, S.8
Christ, F.9
Debyser, Z.10
Neamati, N.11
-
96
-
-
84859850227
-
Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors
-
J. Demeulemeester C. Tintori M. Botta Z. Debyser F. Christ Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors J. Biomol. Screening 2012 17 618 628
-
(2012)
J. Biomol. Screening
, vol.17
, pp. 618-628
-
-
Demeulemeester, J.1
Tintori, C.2
Botta, M.3
Debyser, Z.4
Christ, F.5
-
98
-
-
70349331248
-
An allosteric mechanism for inhibiting HIV-1 integrase with a small molecule
-
J. J. Kessl J. O. Eidahl N. Shkriabai Z. Zhao C. J. McKee S. Hess T. R. Burke Jr. M. Kvaratskhelia An allosteric mechanism for inhibiting HIV-1 integrase with a small molecule Mol. Pharmacol. 2009 76 824 832
-
(2009)
Mol. Pharmacol.
, vol.76
, pp. 824-832
-
-
Kessl, J.J.1
Eidahl, J.O.2
Shkriabai, N.3
Zhao, Z.4
McKee, C.J.5
Hess, S.6
Burke, Jr.T.R.7
Kvaratskhelia, M.8
-
99
-
-
77951294949
-
Crystal structure of the HIV-1 integrase core domain complexed with sucrose reveals details of an allosteric inhibitory binding site
-
J. Wielens S. J. Headey D. Jeevarajah D. I. Rhodes J. Deadman D. K. Chalmers M. J. Scanlon M. W. Parker Crystal structure of the HIV-1 integrase core domain complexed with sucrose reveals details of an allosteric inhibitory binding site FEBS Lett. 2010 584 1455 1462
-
(2010)
FEBS Lett.
, vol.584
, pp. 1455-1462
-
-
Wielens, J.1
Headey, S.J.2
Jeevarajah, D.3
Rhodes, D.I.4
Deadman, J.5
Chalmers, D.K.6
Scanlon, M.J.7
Parker, M.W.8
-
100
-
-
79952330931
-
Structural basis for a new mechanism of inhibition of HIV-1 integrase identified by fragment screening and structure-based design
-
D. I. Rhodes T. S. Peat N. Vandegraaff D. Jeevarajah G. Le E. D. Jones J. A. Smith J. A. Coates L. J. Winfield N. Thienthong J. Newman D. Lucent J. H. Ryan G. P. Savage C. L. Francis J. J. Deadman Structural basis for a new mechanism of inhibition of HIV-1 integrase identified by fragment screening and structure-based design Antiviral Chem. Chemother. 2011 21 155 168
-
(2011)
Antiviral Chem. Chemother.
, vol.21
, pp. 155-168
-
-
Rhodes, D.I.1
Peat, T.S.2
Vandegraaff, N.3
Jeevarajah, D.4
Le, G.5
Jones, E.D.6
Smith, J.A.7
Coates, J.A.8
Winfield, L.J.9
Thienthong, N.10
Newman, J.11
Lucent, D.12
Ryan, J.H.13
Savage, G.P.14
Francis, C.L.15
Deadman, J.J.16
-
101
-
-
53749088987
-
Symmetrical 1-pyrrolidineacetamide showing anti-HIV activity through a new binding site on HIV-1 integrase
-
L. Du Y. X. Zhao L. M. Yang Y. T. Zheng Y. Tang X. Shen H. L. Jiang Symmetrical 1-pyrrolidineacetamide showing anti-HIV activity through a new binding site on HIV-1 integrase Acta Pharmacol. Sin. 2008 29 1261 1267
-
(2008)
Acta Pharmacol. Sin.
, vol.29
, pp. 1261-1267
-
-
Du, L.1
Zhao, Y.X.2
Yang, L.M.3
Zheng, Y.T.4
Tang, Y.5
Shen, X.6
Jiang, H.L.7
-
102
-
-
68149162202
-
Complexes of HIV-1 integrase with HAT proteins: Multiscale models, dynamics, and hypotheses on allosteric sites of inhibition
-
A. Di Fenza W. Rocchia V. Tozzini Complexes of HIV-1 integrase with HAT proteins: multiscale models, dynamics, and hypotheses on allosteric sites of inhibition Proteins 2009 76 946 958
-
(2009)
Proteins
, vol.76
, pp. 946-958
-
-
Di Fenza, A.1
Rocchia, W.2
Tozzini, V.3
-
103
-
-
79251549481
-
Fragment-based design of ligands targeting a novel site on the integrase enzyme of human immunodeficiency virus 1
-
J. Wielens S. J. Headey J. J. Deadman D. I. Rhodes G. T. Le M. W. Parker D. K. Chalmers M. J. Scanlon Fragment-based design of ligands targeting a novel site on the integrase enzyme of human immunodeficiency virus 1 ChemMedChem 2011 6 258 261
-
(2011)
ChemMedChem
, vol.6
, pp. 258-261
-
-
Wielens, J.1
Headey, S.J.2
Deadman, J.J.3
Rhodes, D.I.4
Le, G.T.5
Parker, M.W.6
Chalmers, D.K.7
Scanlon, M.J.8
-
104
-
-
84877959151
-
Rationally designed multitarget anti-HIV agents
-
P. Zhan X. Liu Rationally designed multitarget anti-HIV agents Curr. Med. Chem. 2013 20 1743 1758
-
(2013)
Curr. Med. Chem.
, vol.20
, pp. 1743-1758
-
-
Zhan, P.1
Liu, X.2
-
105
-
-
68449098788
-
Designed multiple ligands: An emerging anti-HIV drug discovery paradigm
-
P. Zhan X. Liu Designed multiple ligands: an emerging anti-HIV drug discovery paradigm Curr. Pharm. Des. 2009 15 1893 1917
-
(2009)
Curr. Pharm. Des.
, vol.15
, pp. 1893-1917
-
-
Zhan, P.1
Liu, X.2
-
106
-
-
84893310295
-
Recent advances in the discovery and development of novel HIV-1 NNRTI platforms (Part II): 2009-2013 update
-
Y. Song Z. Fang P. Zhan X. Liu Recent advances in the discovery and development of novel HIV-1 NNRTI platforms (Part II): 2009-2013 update Curr. Med. Chem. 2013 21 329 355
-
(2013)
Curr. Med. Chem.
, vol.21
, pp. 329-355
-
-
Song, Y.1
Fang, Z.2
Zhan, P.3
Liu, X.4
-
107
-
-
70349395798
-
Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update
-
P. Zhan X. Liu Z. Li Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update Curr. Med. Chem. 2009 16 2876 2889
-
(2009)
Curr. Med. Chem.
, vol.16
, pp. 2876-2889
-
-
Zhan, P.1
Liu, X.2
Li, Z.3
-
108
-
-
84876852661
-
HIV-1 NNRTIs: Structural diversity, pharmacophore similarity, and implications for drug design
-
P. Zhan X. Chen D. Li Z. Fang E. De Clercq X. Liu HIV-1 NNRTIs: Structural diversity, pharmacophore similarity, and implications for drug design Med. Res. Rev. 2013 33 E1 E72
-
(2013)
Med. Res. Rev.
, vol.33
-
-
Zhan, P.1
Chen, X.2
Li, D.3
Fang, Z.4
De Clercq, E.5
Liu, X.6
-
109
-
-
79955104761
-
Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: A patent review (2005-2010)
-
P. Zhan X. Liu Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2005-2010) Expert Opin. Ther. Pat. 2011 21 717 796
-
(2011)
Expert Opin. Ther. Pat.
, vol.21
, pp. 717-796
-
-
Zhan, P.1
Liu, X.2
-
111
-
-
34547583281
-
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase
-
Z. Wang E. M. Bennett D. J. Wilson C. Salomon R. Vince Rationally designed dual inhibitors of HIV reverse transcriptase and integrase J. Med. Chem. 2007 50 3416 3419
-
(2007)
J. Med. Chem.
, vol.50
, pp. 3416-3419
-
-
Wang, Z.1
Bennett, E.M.2
Wilson, D.J.3
Salomon, C.4
Vince, R.5
-
112
-
-
77953127859
-
Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase
-
Z. Wang J. Tang C. E. Salomon C. D. Dreis R. Vince Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase Bioorg. Med. Chem. 2010 18 4202 4211
-
(2010)
Bioorg. Med. Chem.
, vol.18
, pp. 4202-4211
-
-
Wang, Z.1
Tang, J.2
Salomon, C.E.3
Dreis, C.D.4
Vince, R.5
-
113
-
-
78651481692
-
N-3 Hydroxylation of pyrimidine-2,4-diones yields dual inhibitors of HIV reverse transcriptase and integrase
-
J. Tang K. Maddali C. D. Dreis Y. Y. Sham R. Vince Y. Pommier Z. Wang N-3 Hydroxylation of pyrimidine-2,4-diones yields dual inhibitors of HIV reverse transcriptase and integrase ACS Med. Chem. Lett. 2011 2 63 67
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 63-67
-
-
Tang, J.1
Maddali, K.2
Dreis, C.D.3
Sham, Y.Y.4
Vince, R.5
Pommier, Y.6
Wang, Z.7
-
114
-
-
79953784039
-
3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase
-
J. Tang K. Maddali M. Metifiot Y. Y. Sham R. Vince Y. Pommier Z. Wang 3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase J. Med. Chem. 2011 54 2282 2292
-
(2011)
J. Med. Chem.
, vol.54
, pp. 2282-2292
-
-
Tang, J.1
Maddali, K.2
Metifiot, M.3
Sham, Y.Y.4
Vince, R.5
Pommier, Y.6
Wang, Z.7
-
115
-
-
79953276335
-
6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase
-
J. Tang K. Maddali C. D. Dreis Y. Y. Sham R. Vince Y. Pommier Z. Wang 6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase Bioorg. Med. Chem. Lett. 2011 21 2400 2402
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 2400-2402
-
-
Tang, J.1
Maddali, K.2
Dreis, C.D.3
Sham, Y.Y.4
Vince, R.5
Pommier, Y.6
Wang, Z.7
-
116
-
-
84877987020
-
Multivalent agents: A novel concept and preliminary practice in Anti-HIV drug discovery
-
Y. Song P. Zhan X. Li D. Rai E. De Clercq X. Liu Multivalent agents: a novel concept and preliminary practice in Anti-HIV drug discovery Curr. Med. Chem. 2013 20 815 832
-
(2013)
Curr. Med. Chem.
, vol.20
, pp. 815-832
-
-
Song, Y.1
Zhan, P.2
Li, X.3
Rai, D.4
De Clercq, E.5
Liu, X.6
-
117
-
-
84878044985
-
Bifunctional inhibition of human immunodeficiency virus type 1 reverse transcriptase: Mechanism and proof-of-concept as a novel therapeutic design strategy
-
C. M. Bailey T. J. Sullivan P. Iyidogan J. Tirado-Rives R. Chung J. Ruiz-Caro E. Mohamed W. Jorgensen R. Hunter K. S. Anderson Bifunctional inhibition of human immunodeficiency virus type 1 reverse transcriptase: mechanism and proof-of-concept as a novel therapeutic design strategy J. Med. Chem. 2013 56 3959 3968
-
(2013)
J. Med. Chem.
, vol.56
, pp. 3959-3968
-
-
Bailey, C.M.1
Sullivan, T.J.2
Iyidogan, P.3
Tirado-Rives, J.4
Chung, R.5
Ruiz-Caro, J.6
Mohamed, E.7
Jorgensen, W.8
Hunter, R.9
Anderson, K.S.10
-
118
-
-
77949858836
-
Kinetic target-guided synthesis
-
X. Hu R. Manetsch Kinetic target-guided synthesis Chem. Soc. Rev. 2010 39 1316 1324
-
(2010)
Chem. Soc. Rev.
, vol.39
, pp. 1316-1324
-
-
Hu, X.1
Manetsch, R.2
-
119
-
-
84877835595
-
Click chemistry for drug development and diverse chemical-biology applications
-
P. Thirumurugan D. Matosiuk K. Jozwiak Click chemistry for drug development and diverse chemical-biology applications Chem. Rev. 2013 113 4905 4979
-
(2013)
Chem. Rev.
, vol.113
, pp. 4905-4979
-
-
Thirumurugan, P.1
Matosiuk, D.2
Jozwiak, K.3
-
120
-
-
33746210083
-
Inhibitors of HIV-1 protease by using in situ click chemistry
-
M. Whiting J. Muldoon Y. C. Lin S. M. Silverman W. Lindstrom A. J. Olson H. C. Kolb M. G. Finn K. B. Sharpless J. H. Elder V. V. Fokin Inhibitors of HIV-1 protease by using in situ click chemistry Angew. Chem., Int. Ed. 2006 45 1435 1439
-
(2006)
Angew. Chem., Int. Ed.
, vol.45
, pp. 1435-1439
-
-
Whiting, M.1
Muldoon, J.2
Lin, Y.C.3
Silverman, S.M.4
Lindstrom, W.5
Olson, A.J.6
Kolb, H.C.7
Finn, M.G.8
Sharpless, K.B.9
Elder, J.H.10
Fokin, V.V.11
-
121
-
-
0345306644
-
Rapid diversity-oriented synthesis in microtiter plates for in situ screening of HIV protease inhibitors
-
A. Brik J. Muldoon Y. C. Lin J. H. Elder D. S. Goodsell A. J. Olson V. V. Fokin K. B. Sharpless C. H. Wong Rapid diversity-oriented synthesis in microtiter plates for in situ screening of HIV protease inhibitors ChemBioChem 2003 4 1246 1248
-
(2003)
ChemBioChem
, vol.4
, pp. 1246-1248
-
-
Brik, A.1
Muldoon, J.2
Lin, Y.C.3
Elder, J.H.4
Goodsell, D.S.5
Olson, A.J.6
Fokin, V.V.7
Sharpless, K.B.8
Wong, C.H.9
-
123
-
-
1942453243
-
Ligand efficiency: A useful metric for lead selection
-
A. L. Hopkins C. R. Groom A. Alex Ligand efficiency: a useful metric for lead selection Drug Discovery Today 2004 9 430 431
-
(2004)
Drug Discovery Today
, vol.9
, pp. 430-431
-
-
Hopkins, A.L.1
Groom, C.R.2
Alex, A.3
-
124
-
-
69949092805
-
Pyrazole NNRTIs 1: Design and initial optimisation of a novel template
-
C. E. Mowbray C. Burt R. Corbau M. Perros I. Tran P. A. Stupple R. Webster A. Wood Pyrazole NNRTIs 1: design and initial optimisation of a novel template Bioorg. Med. Chem. Lett. 2009 19 5599 5602
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 5599-5602
-
-
Mowbray, C.E.1
Burt, C.2
Corbau, R.3
Perros, M.4
Tran, I.5
Stupple, P.A.6
Webster, R.7
Wood, A.8
-
125
-
-
69949108856
-
Pyrazole NNRTIs 3: Optimisation of physicochemical properties
-
C. E. Mowbray R. Corbau M. Hawes L. H. Jones J. E. Mills M. Perros M. D. Selby P. A. Stupple R. Webster A. Wood Pyrazole NNRTIs 3: optimisation of physicochemical properties Bioorg. Med. Chem. Lett. 2009 19 5603 5606
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 5603-5606
-
-
Mowbray, C.E.1
Corbau, R.2
Hawes, M.3
Jones, L.H.4
Mills, J.E.5
Perros, M.6
Selby, M.D.7
Stupple, P.A.8
Webster, R.9
Wood, A.10
-
126
-
-
70349214797
-
Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a development candidate
-
C. E. Mowbray C. Burt R. Corbau S. Gayton M. Hawes M. Perros I. Tran D. A. Price F. J. Quinton M. D. Selby P. A. Stupple R. Webster A. Wood Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate Bioorg. Med. Chem. Lett. 2009 19 5857 5860
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 5857-5860
-
-
Mowbray, C.E.1
Burt, C.2
Corbau, R.3
Gayton, S.4
Hawes, M.5
Perros, M.6
Tran, I.7
Price, D.A.8
Quinton, F.J.9
Selby, M.D.10
Stupple, P.A.11
Webster, R.12
Wood, A.13
-
127
-
-
77950922576
-
Activity, pharmacokinetics and safety of lersivirine (UK-453,061), a next-generation nonnucleoside reverse transcriptase inhibitor, during 7-day monotherapy in HIV-1-infected patients
-
G. Fätkenheuer S. Staszewski A. Plettenburg F. Hackman G. Layton L. McFadyen J. Davis T. M. Jenkins Activity, pharmacokinetics and safety of lersivirine (UK-453,061), a next-generation nonnucleoside reverse transcriptase inhibitor, during 7-day monotherapy in HIV-1-infected patients AIDS 2009 23 2115 2122
-
(2009)
AIDS
, vol.23
, pp. 2115-2122
-
-
Fätkenheuer, G.1
Staszewski, S.2
Plettenburg, A.3
Hackman, F.4
Layton, G.5
McFadyen, L.6
Davis, J.7
Jenkins, T.M.8
-
128
-
-
77957370457
-
Lersivirine: A non-nucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus-1
-
R. Corbau J. Mori C. Phillips L. Fishburn A. Martin C. Mowbray W. Panton C. Smith-Burchnell A. Thornberry H. Ringrose T. Knöchel S. Irving M. Westby A. Wood M. Perros Lersivirine: a non-nucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus-1 Antimicrob. Agents Chemother. 2010 54 4451 4463
-
(2010)
Antimicrob. Agents Chemother.
, vol.54
, pp. 4451-4463
-
-
Corbau, R.1
Mori, J.2
Phillips, C.3
Fishburn, L.4
Martin, A.5
Mowbray, C.6
Panton, W.7
Smith-Burchnell, C.8
Thornberry, A.9
Ringrose, H.10
Knöchel, T.11
Irving, S.12
Westby, M.13
Wood, A.14
Perros, M.15
-
129
-
-
80054892853
-
Combined approach using ligand efficiency, cross-docking, and antitarget hits for wild-type and drug-resistant Y181C HIV-1 reverse transcriptase
-
A. T. García-Sosa S. Sild K. Takkis U. Maran Combined approach using ligand efficiency, cross-docking, and antitarget hits for wild-type and drug-resistant Y181C HIV-1 reverse transcriptase J. Chem. Inf. Model. 2011 51 2595 2611
-
(2011)
J. Chem. Inf. Model.
, vol.51
, pp. 2595-2611
-
-
García-Sosa, A.T.1
Sild, S.2
Takkis, K.3
Maran, U.4
-
130
-
-
64349086788
-
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays
-
L. H. Jones G. Allan O. Barba C. Burt R. Corbau T. Dupont T. Knöchel S. Irving D. S. Middleton C. E. Mowbray M. Perros H. Ringrose N. A. Swain R. Webster M. Westby C. Phillips Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays J. Med. Chem. 2009 52 1219 1223
-
(2009)
J. Med. Chem.
, vol.52
, pp. 1219-1223
-
-
Jones, L.H.1
Allan, G.2
Barba, O.3
Burt, C.4
Corbau, R.5
Dupont, T.6
Knöchel, T.7
Irving, S.8
Middleton, D.S.9
Mowbray, C.E.10
Perros, M.11
Ringrose, H.12
Swain, N.A.13
Webster, R.14
Westby, M.15
Phillips, C.16
-
131
-
-
84890465064
-
Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins
-
Y. Tanaka K. Aikawa G. Nishida M. Homma S. Sogabe S. Igaki Y. Hayano T. Sameshima I. Miyahisa T. Kawamoto M. Tawada Y. Imai M. Inazuka N. Cho Y. Imaeda T. Ishikawa Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins J. Med. Chem. 2013 56 9635 9645
-
(2013)
J. Med. Chem.
, vol.56
, pp. 9635-9645
-
-
Tanaka, Y.1
Aikawa, K.2
Nishida, G.3
Homma, M.4
Sogabe, S.5
Igaki, S.6
Hayano, Y.7
Sameshima, T.8
Miyahisa, I.9
Kawamoto, T.10
Tawada, M.11
Imai, Y.12
Inazuka, M.13
Cho, N.14
Imaeda, Y.15
Ishikawa, T.16
-
132
-
-
84859774923
-
Potent and selective inhibitors of CK2 kinase identified through structure-guided hybridization
-
J. E. Dowling C. Chuaqui T. W. Pontz P. D. Lyne N. A. Larsen M. H. Block H. Chen N. Su A. Wu D. Russell H. Pollard J. W. Lee B. Peng K. Thakur Q. Ye T. Zhang P. Brassil V. Racicot L. Bao C. R. Denz E. Cooke Potent and selective inhibitors of CK2 kinase identified through structure-guided hybridization ACS Med. Chem. Lett. 2012 3 278 283
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 278-283
-
-
Dowling, J.E.1
Chuaqui, C.2
Pontz, T.W.3
Lyne, P.D.4
Larsen, N.A.5
Block, M.H.6
Chen, H.7
Su, N.8
Wu, A.9
Russell, D.10
Pollard, H.11
Lee, J.W.12
Peng, B.13
Thakur, K.14
Ye, Q.15
Zhang, T.16
Brassil, P.17
Racicot, V.18
Bao, L.19
Denz, C.R.20
Cooke, E.21
more..
-
133
-
-
84890495266
-
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors
-
H. Huang A. Guzman-Perez L. Acquaviva V. Berry H. Bregman J. Dovey H. Gunaydin X. Huang L. Huang D. Saffran R. Serafino S. Schneider C. Wilson E. F. DiMauro Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors ACS Med. Chem. Lett. 2013 4 1218 1223
-
(2013)
ACS Med. Chem. Lett.
, vol.4
, pp. 1218-1223
-
-
Huang, H.1
Guzman-Perez, A.2
Acquaviva, L.3
Berry, V.4
Bregman, H.5
Dovey, J.6
Gunaydin, H.7
Huang, X.8
Huang, L.9
Saffran, D.10
Serafino, R.11
Schneider, S.12
Wilson, C.13
Dimauro, E.F.14
-
134
-
-
84879040140
-
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors
-
H. Bregman N. Chakka A. Guzman-Perez H. Gunaydin Y. Gu X. Huang V. Berry J. Liu Y. Teffera L. Huang B. Egge E. L. Mullady S. Schneider P. S. Andrews A. Mishra J. Newcomb R. Serafino C. A. Strathdee S. M. Turci C. Wilson E. F. DiMauro Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors J. Med. Chem. 2013 56 4320 4342
-
(2013)
J. Med. Chem.
, vol.56
, pp. 4320-4342
-
-
Bregman, H.1
Chakka, N.2
Guzman-Perez, A.3
Gunaydin, H.4
Gu, Y.5
Huang, X.6
Berry, V.7
Liu, J.8
Teffera, Y.9
Huang, L.10
Egge, B.11
Mullady, E.L.12
Schneider, S.13
Andrews, P.S.14
Mishra, A.15
Newcomb, J.16
Serafino, R.17
Strathdee, C.A.18
Turci, S.M.19
Wilson, C.20
Dimauro, E.F.21
more..
-
135
-
-
84903710585
-
Old friends in new guise: Exploiting privileged structures for scaffold re-evolution/refining
-
10.2174/1386207317666140122101631, Epub ahead of print
-
Y. Song W. Chen D. Kang Q. Zhang P. Zhan X. Liu "Old friends in new guise": exploiting privileged structures for scaffold re-evolution/refining Comb. Chem. High Throughput Screening 2014 10.2174/1386207317666140122101631
-
(2014)
Comb. Chem. High Throughput Screening
-
-
Song, Y.1
Chen, W.2
Kang, D.3
Zhang, Q.4
Zhan, P.5
Liu, X.6
-
137
-
-
84858141881
-
Combining biophysical screening and X-ray crystallography for fragment-based drug discovery
-
M. Hennig A. Ruf W. Huber Combining biophysical screening and X-ray crystallography for fragment-based drug discovery Top. Curr. Chem. 2012 317 115 143
-
(2012)
Top. Curr. Chem.
, vol.317
, pp. 115-143
-
-
Hennig, M.1
Ruf, A.2
Huber, W.3
|