-
1
-
-
2942527726
-
HIV-1 integrase: A target for new AIDS chemotherapeutics
-
Anthony, N. J. HIV-1 integrase: A target for new AIDS chemotherapeutics Curr. Top. Med. Chem. 2004, 4, 979-990
-
(2004)
Curr. Top. Med. Chem.
, vol.4
, pp. 979-990
-
-
Anthony, N.J.1
-
2
-
-
42049119625
-
Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro
-
Malet, I.; Delelis, O.; Valantin, M. A.; Montes, B.; Soulie, C.; Wirden, M.; Tchertanov, L.; Peytavin, G.; Reynes, J.; Mouscadet, J. F.; Katlama, C.; Calvez, V.; Marcelin, A. G. Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro Antimicrob. Agents Chemother. 2008, 52, 1351-1358
-
(2008)
Antimicrob. Agents Chemother.
, vol.52
, pp. 1351-1358
-
-
Malet, I.1
Delelis, O.2
Valantin, M.A.3
Montes, B.4
Soulie, C.5
Wirden, M.6
Tchertanov, L.7
Peytavin, G.8
Reynes, J.9
Mouscadet, J.F.10
Katlama, C.11
Calvez, V.12
Marcelin, A.G.13
-
3
-
-
77957875432
-
Specific HIV-1 integrase polymorphisms change their prevalence in untreated versus antiretroviral-treated HIV-1-infected patients, all naive to integrase inhibitors
-
Ceccherini-Silberstein, F.; Malet, I.; Fabeni, L.; Dimonte, S.; Svicher, V.; D'Arrigo, R.; Artese, A.; Costa, G.; Bono, S.; Alcaro, S.; Monforte, A.; Katlama, C.; Calvez, V.; Antinori, A.; Marcelin, A. G.; Perno, C. F. Specific HIV-1 integrase polymorphisms change their prevalence in untreated versus antiretroviral-treated HIV-1-infected patients, all naive to integrase inhibitors J. Antimicrob. Chemother. 2010, 65, 2305-2318
-
(2010)
J. Antimicrob. Chemother.
, vol.65
, pp. 2305-2318
-
-
Ceccherini-Silberstein, F.1
Malet, I.2
Fabeni, L.3
Dimonte, S.4
Svicher, V.5
D'Arrigo, R.6
Artese, A.7
Costa, G.8
Bono, S.9
Alcaro, S.10
Monforte, A.11
Katlama, C.12
Calvez, V.13
Antinori, A.14
Marcelin, A.G.15
Perno, C.F.16
-
4
-
-
79251545504
-
Allosteric inhibitor development targeting HIV-1 integrase
-
Al-Mawsawi, L. Q.; Neamati, N. 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
-
5
-
-
3142781225
-
Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream
-
Arkin, M. R.; Wells, J. A. Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream Nat. Rev. Drug Discovery 2004, 3, 301-317
-
(2004)
Nat. Rev. Drug Discovery
, vol.3
, pp. 301-317
-
-
Arkin, M.R.1
Wells, J.A.2
-
6
-
-
0346733329
-
Are protein-protein interfaces more conserved in sequence than the rest of the protein surface?
-
Caffrey, D. R.; Somaroo, S.; Hughes, J. D.; Mintseris, J.; Huang, E. S. Are protein-protein interfaces more conserved in sequence than the rest of the protein surface? Protein Sci. 2004, 13, 190-202
-
(2004)
Protein Sci.
, vol.13
, pp. 190-202
-
-
Caffrey, D.R.1
Somaroo, S.2
Hughes, J.D.3
Mintseris, J.4
Huang, E.S.5
-
7
-
-
33947173624
-
Inhibitors of Protein-Protein Interactions as Potential Drugs
-
Veselovsky, A. V.; Archakov, A. I. Inhibitors of Protein-Protein Interactions as Potential Drugs Curr. Comput.-Aided Drug Des. 2007, 3, 51-58
-
(2007)
Curr. Comput.-Aided Drug Des.
, vol.3
, pp. 51-58
-
-
Veselovsky, A.V.1
Archakov, A.I.2
-
8
-
-
37249004920
-
Reaching for high-hanging fruit in drug discovery at protein-protein interfaces
-
Wells, J. A.; McClendon, C. L. Reaching for high-hanging fruit in drug discovery at protein-protein interfaces Nature 2007, 450, 1001-1009
-
(2007)
Nature
, vol.450
, pp. 1001-1009
-
-
Wells, J.A.1
McClendon, C.L.2
-
9
-
-
32344452179
-
Cellular co-factors of HIV-1 integration
-
Van Maele, B.; Busschots, K.; Vandekerckhove, L.; Christ, F.; Debyser, Z. Cellular co-factors of HIV-1 integration Trends Biochem. Sci. 2006, 31, 98-105
-
(2006)
Trends Biochem. Sci.
, vol.31
, pp. 98-105
-
-
Van Maele, B.1
Busschots, K.2
Vandekerckhove, L.3
Christ, F.4
Debyser, Z.5
-
10
-
-
0346036088
-
HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells
-
Cherepanov, P.; Maertens, G.; Proost, P.; Devreese, B.; Van Beeumen, J.; Engelborghs, Y.; De Clercq, E. Debyser, Z. HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells J. Biol. Chem. 2003, 278, 372-381
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 372-381
-
-
Cherepanov, P.1
Maertens, G.2
Proost, P.3
Devreese, B.4
Van Beeumen, J.5
Engelborghs, Y.6
De Clercq, E.7
Debyser, Z.8
-
11
-
-
28644443483
-
A role for LEDGF/p75 in targeting HIV DNA integration
-
Ciuffi, A.; Llano, M.; Poeschla, E.; Hoffmann, C.; Leipzig, J.; Shinn, P.; Ecker, J. R.; Bushman, F. A role for LEDGF/p75 in targeting HIV DNA integration Nat. Med. 2005, 11, 1287-1289
-
(2005)
Nat. Med.
, vol.11
, pp. 1287-1289
-
-
Ciuffi, A.1
Llano, M.2
Poeschla, E.3
Hoffmann, C.4
Leipzig, J.5
Shinn, P.6
Ecker, J.R.7
Bushman, F.8
-
12
-
-
33750358735
-
An essential role for LEDGF/p75 in HIV integration
-
Llano, M.; Saenz, D. T.; Meehan, A.; Wongthida, P.; Peretz, M.; Walker, W. H.; Teo, W. L.; Poeschla, E. M. An essential role for LEDGF/p75 in HIV integration Science 2006, 314, 461-464
-
(2006)
Science
, vol.314
, pp. 461-464
-
-
Llano, M.1
Saenz, D.T.2
Meehan, A.3
Wongthida, P.4
Peretz, M.5
Walker, W.H.6
Teo, W.L.7
Poeschla, E.M.8
-
13
-
-
33745745419
-
Retroviral DNA integration: HIV and the role of LEDGF/p75
-
Ciuffi, A.; Bushman, F. D. Retroviral DNA integration: HIV and the role of LEDGF/p75 Trends Genet. 2006, 22, 388-395
-
(2006)
Trends Genet.
, vol.22
, pp. 388-395
-
-
Ciuffi, A.1
Bushman, F.D.2
-
14
-
-
34748852513
-
Blocking interactions between HIV-1 integrase and cellular cofactors: An emerging anti-retroviral strategy
-
Al-Mawsawi, L. Q.; Neamati, N. Blocking interactions between HIV-1 integrase and cellular cofactors: an emerging anti-retroviral strategy Trends Pharmacol. Sci. 2007, 28, 526-535
-
(2007)
Trends Pharmacol. Sci.
, vol.28
, pp. 526-535
-
-
Al-Mawsawi, L.Q.1
Neamati, N.2
-
15
-
-
43049182995
-
Integrase, LEDGF/p75 and HIV replication
-
Poeschla, E. M. Integrase, LEDGF/p75 and HIV replication Cell. Mol. Life Sci. 2008, 65, 1403-1424
-
(2008)
Cell. Mol. Life Sci.
, vol.65
, pp. 1403-1424
-
-
Poeschla, E.M.1
-
16
-
-
33751242046
-
Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication
-
De Rijck, J.; Vandekerckhove, L.; Gijsbers, R.; Hombrouck, A.; Hendrix, J.; Vercammen, J.; Engelborghs, Y.; Christ, F.; Debyser, Z. Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication J. Virol. 2006, 80, 11498-11509
-
(2006)
J. Virol.
, vol.80
, pp. 11498-11509
-
-
De Rijck, J.1
Vandekerckhove, L.2
Gijsbers, R.3
Hombrouck, A.4
Hendrix, J.5
Vercammen, J.6
Engelborghs, Y.7
Christ, F.8
Debyser, Z.9
-
17
-
-
34047200871
-
Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV
-
Hombrouck, A.; De Rijck, J.; Hendrix, J.; Vandekerckhove, L.; Voet, A.; De Maeyer, M.; Witvrouw, M.; Engelborghs, Y.; Christ, F.; Gijsbers, R.; Debyser, Z. Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV PLoS Pathog. 2007, 3, e47
-
(2007)
PLoS Pathog.
, vol.3
, pp. 47
-
-
Hombrouck, A.1
De Rijck, J.2
Hendrix, J.3
Vandekerckhove, L.4
Voet, A.5
De Maeyer, M.6
Witvrouw, M.7
Engelborghs, Y.8
Christ, F.9
Gijsbers, R.10
Debyser, Z.11
-
18
-
-
50149096422
-
D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75
-
Du, L.; Zhao, Y. X.; Chen, J.; Yang, L. M.; Zheng, Y. T.; Tang, Y.; Shen, X.; Jiang, H. L. 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.X.2
Chen, J.3
Yang, L.M.4
Zheng, Y.T.5
Tang, Y.6
Shen, X.7
Jiang, H.L.8
-
19
-
-
68149149956
-
Pharmacophore-Based Discovery of Small-Molecule Inhibitors of Protein-Protein Interactions between HIV-1 Integrase and Cellular Cofactor LEDGF/p75
-
De Luca, L.; Barreca, M. L.; Ferro, S.; Christ, F.; Iraci, N.; Gitto, R.; Monforte, A. M.; Debyser, Z.; Chimirri, A. 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
-
20
-
-
77958015795
-
Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor
-
De Luca, L.; Ferro, S.; Gitto, R.; Barreca, M. L.; Agnello, S.; Christ, F.; Debyser, Z.; Chimirri, A. 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
-
21
-
-
77952553431
-
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication
-
Christ, F.; Voet, A.; Marchand, A.; Nicolet, S.; Desimmie, B. A.; Marchand, D.; Bardiot, D.; Van der Veken, N. J.; Van Remoortel, B.; Strelkov, S. V.; De Maeyer, M.; Chaltin, P.; Debyser, Z. 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
Van Der Veken, N.J.8
Van Remoortel, B.9
Strelkov, S.V.10
De Maeyer, M.11
Chaltin, P.12
Debyser, Z.13
-
22
-
-
84862271587
-
New class of HIV-1 integrase (IN) inhibitors with a dual mode of action
-
Tsiang, M.; Jones, G. S.; Niedziela-Majka, A.; Kan, E.; Lansdon, E. B.; Huang, W.; Hung, M.; Samuel, D.; Novikov, N.; Xu, Y.; Mitchell, M.; Guo, H.; Babaoglu, K.; Liu, X.; Geleziunas, R.; Sakowicz, R. 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
-
23
-
-
84864387134
-
Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization
-
Christ, F.; Shaw, S.; Demeulemeester, J.; Desimmie, B. A.; Marchand, A.; Butler, S.; Smets, W.; Chaltin, P.; Westby, M.; Debyser, Z.; Pickford, C. 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
-
24
-
-
52049109838
-
Natural products in drug discovery
-
Harvey, A. L. Natural products in drug discovery Drug Discovery Today 2008, 13, 894-901
-
(2008)
Drug Discovery Today
, vol.13
, pp. 894-901
-
-
Harvey, A.L.1
-
25
-
-
0034649618
-
Protein-based virtual screening of chemical databases. 1. Evaluation of different docking/scoring combinations
-
Bissantz, C.; Folkers, G.; Rognan, D. Protein-based virtual screening of chemical databases. 1. Evaluation of different docking/scoring combinations J. Med. Chem. 2000, 43, 4759-4767
-
(2000)
J. Med. Chem.
, vol.43
, pp. 4759-4767
-
-
Bissantz, C.1
Folkers, G.2
Rognan, D.3
-
26
-
-
74049133612
-
Optimal assignment methods for ligand-based virtual screening
-
Jahn, A.; Hinselmann, G.; Fechner, N.; Zell, A. Optimal assignment methods for ligand-based virtual screening J. Cheminform. 2009, 1, 14
-
(2009)
J. Cheminform.
, vol.1
, pp. 14
-
-
Jahn, A.1
Hinselmann, G.2
Fechner, N.3
Zell, A.4
-
27
-
-
44849094570
-
Screening for antiviral inhibitors of the HIV integrase - LEDGF/p75 interaction using the AlphaScreen (TM) luminescent proximity assay
-
Hou, Y.; McGuinness, D. E.; Prongay, A. J.; Feld, B.; Ingravallo, P.; Ogert, R. A.; Lunn, C. A.; Howe, J. A. Screening for antiviral inhibitors of the HIV integrase-LEDGF/p75 interaction using the AlphaScreen (TM) luminescent proximity assay J. Biomol. Screening 2008, 13, 406-414
-
(2008)
J. Biomol. Screening
, vol.13
, pp. 406-414
-
-
Hou, Y.1
McGuinness, D.E.2
Prongay, A.J.3
Feld, B.4
Ingravallo, P.5
Ogert, R.A.6
Lunn, C.A.7
Howe, J.A.8
-
28
-
-
84871059378
-
-
version 3.4, Schrödinger, LLC, New York, NY.
-
QikProp, version 3.4, Schrödinger, LLC, New York, NY, 2011.
-
(2011)
QikProp
-
-
-
29
-
-
28444445583
-
Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75
-
Cherepanov, P.; Ambrosio, A. L. B.; Rahman, S.; Ellenberger, T.; Engelman, A. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75 Proc. Natl. Acad. Sci. U.S.A. 2005, 102, 17308-17313
-
(2005)
Proc. Natl. Acad. Sci. U.S.A.
, vol.102
, pp. 17308-17313
-
-
Cherepanov, P.1
Ambrosio, A.L.B.2
Rahman, S.3
Ellenberger, T.4
Engelman, A.5
-
30
-
-
33846049539
-
Identification of the LEDGF/p75 binding site in HIV-1 integrase
-
Busschots, K.; Voet, A.; De Maeyer, M.; Rain, J. C.; Emiliani, S.; Benarous, R.; Desender, L.; Debyser, Z.; Christ, F. Identification of the LEDGF/p75 binding site in HIV-1 integrase J. Mol. Biol. 2007, 365, 1480-1492
-
(2007)
J. Mol. Biol.
, vol.365
, pp. 1480-1492
-
-
Busschots, K.1
Voet, A.2
De Maeyer, M.3
Rain, J.C.4
Emiliani, S.5
Benarous, R.6
Desender, L.7
Debyser, Z.8
Christ, F.9
-
31
-
-
84871064769
-
-
version 2.1, Schrödinger, LLC, New York, NY.
-
Prime, version 2.1, Schrödinger, LLC, New York, NY, 2009.
-
(2009)
Prime
-
-
-
32
-
-
84871036749
-
-
version 5.5, Schrödinger, LLC, New York, NY.
-
Glide, version 5.5, Schrödinger, LLC, New York, NY, 2009.
-
(2009)
Glide
-
-
-
33
-
-
84871066809
-
-
version 2.3, Schrödinger, LLC, New York, NY.
-
LigPrep, version 2.3, Schrödinger, LLC, New York, NY, 2009.
-
(2009)
LigPrep
-
-
-
34
-
-
12144289984
-
Glide: A new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy
-
Friesner, R. A.; Banks, J. L.; Murphy, R. B.; Halgren, T. A.; Klicic, J. J.; Mainz, D. T.; Repasky, M. P.; Knoll, E. H.; Shelley, M.; Perry, J. K.; Shaw, D. E.; Francis, P.; Shenkin, P. S. Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy J. Med. Chem. 2004, 47, 1739-1749
-
(2004)
J. Med. Chem.
, vol.47
, pp. 1739-1749
-
-
Friesner, R.A.1
Banks, J.L.2
Murphy, R.B.3
Halgren, T.A.4
Klicic, J.J.5
Mainz, D.T.6
Repasky, M.P.7
Knoll, E.H.8
Shelley, M.9
Perry, J.K.10
Shaw, D.E.11
Francis, P.12
Shenkin, P.S.13
-
35
-
-
77953326788
-
Chemical space sampling by different scoring functions and crystal structures
-
Brooijmans, N.; Humblet, C. Chemical space sampling by different scoring functions and crystal structures J. Comput.-Aided Mol. Des. 2010, 24, 433-447
-
(2010)
J. Comput.-Aided Mol. Des.
, vol.24
, pp. 433-447
-
-
Brooijmans, N.1
Humblet, C.2
-
36
-
-
51449111044
-
Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities
-
Zhang, Y. N.; Zhang, W.; Hong, D.; Shi, L.; Shen, Q.; Li, J. Y.; Li, J.; Hu, L. H. Oleanolic acid and its derivatives: new inhibitor of protein tyrosine phosphatase 1B with cellular activities Bioorg. Med. Chem. 2008, 16, 8697-8705
-
(2008)
Bioorg. Med. Chem.
, vol.16
, pp. 8697-8705
-
-
Zhang, Y.N.1
Zhang, W.2
Hong, D.3
Shi, L.4
Shen, Q.5
Li, J.Y.6
Li, J.7
Hu, L.H.8
-
37
-
-
80052850006
-
Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1)
-
Ma, L.; Yang, Z.; Li, C.; Zhu, Z.; Shen, X.; Hu, L. Design, synthesis and SAR study of hydroxychalcone inhibitors of human beta-secretase (BACE1) J. Enzyme Inhib. Med. Chem. 2011, 26, 643-648
-
(2011)
J. Enzyme Inhib. Med. Chem.
, vol.26
, pp. 643-648
-
-
Ma, L.1
Yang, Z.2
Li, C.3
Zhu, Z.4
Shen, X.5
Hu, L.6
-
38
-
-
0029980485
-
A soluble active mutant of HIV-1 integrase: Involvement of both the core and carboxyl-terminal domains in multimerization
-
Jenkins, T. M.; Engelman, A.; Ghirlando, R.; Craigie, R. A soluble active mutant of HIV-1 integrase: involvement of both the core and carboxyl-terminal domains in multimerization J. Biol. Chem. 1996, 271, 7712-7718
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 7712-7718
-
-
Jenkins, T.M.1
Engelman, A.2
Ghirlando, R.3
Craigie, R.4
-
39
-
-
0028949396
-
In vitro immunotoxicity and cytotoxicity of trichosanthin against human normal immunocytes and leukemia-lymphoma cells
-
Zheng, Y. T.; Zhang, W. F.; Ben, K. L.; Wang, J. H. In vitro immunotoxicity and cytotoxicity of trichosanthin against human normal immunocytes and leukemia-lymphoma cells Immunopharmacol. Immunotoxicol. 1995, 17, 69-79
-
(1995)
Immunopharmacol. Immunotoxicol.
, vol.17
, pp. 69-79
-
-
Zheng, Y.T.1
Zhang, W.F.2
Ben, K.L.3
Wang, J.H.4
|