Retroviral integrase inhibitors year 2000: update and perspectives

被引：98

作者：

Pommier, Y ^{[1
]}

Marchand, C ^{[1
]}

Neamati, N ^{[1
]}

机构：

[1] NCI, Div Basic Sci, Mol Pharmacol Lab, Bethesda, MD 20892 USA

来源：

ANTIVIRAL RESEARCH | 2000年 / 47卷 / 03期

基金：

美国国家卫生研究院;

关键词：

retroviruses; integrase inhibitors; resistance; structure of integrases;

D O I：

10.1016/S0166-3542(00)00112-1

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

HIV-1 integrase is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. A number of inhibitors have been reported in the past 8 years. This review focuses on the recent developments in the past 2 years. There are now several inhibitors with known sites of actions and antiviral activity. The challenge is to convert these leads into drugs that will selectively target integrase in vivo, and can be added to our antiviral armamentarium. (C) 2000 Published by Elsevier Science B.V.

引用

页码：139 / 148

页数：10

共 57 条

[1] The plant ribosome inactivating proteins luffin and saporin are potent inhibitors of HIV-1 integrase [J].

Au, TK ;

Collins, RA ;

Lam, TL ;

Ng, TB ;

Fong, WP ;

Wan, DCC .

FEBS LETTERS, 2000, 471 (2-3) :169-172

[2] Alternate strand DNA triple helix-mediated inhibition of HIV-1 U5 long terminal repeat integration in vitro [J].

Bouziane, M ;

Cherny, DI ;

Mouscadet, JF ;

Auclair, C .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (17) :10359-10364

[3] Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase [J].

Brodin, P ;

Pinskaya, M ;

Volkov, E ;

Romanova, E ;

Leh, H ;

Auclair, C ;

Mouscadet, JF ;

Gottikh, M .

FEBS LETTERS, 1999, 460 (02) :270-274

[4] SENSITIVITY OF HIV-1 REVERSE-TRANSCRIPTASE AND ITS MUTANTS TO INHIBITION BY AZIDOTHYMIDINE TRIPHOSPHATE [J].

CARROLL, SS ;

GEIB, J ;

OLSEN, DB ;

STAHLHUT, M ;

SHAFER, JA ;

KUO, LC .

BIOCHEMISTRY, 1994, 33 (08) :2113-2120

[5] High affinity interaction of HIV-1 integrase with specific and non-specific single-stranded short oligonucleotides [J].

Caumont, A ;

Jamieson, G ;

de Soultrait, VR ;

Parissi, V ;

Fournier, M ;

Zakharova, OD ;

Bayandin, R ;

Litvak, S ;

Tarrago-Litvak, L ;

Nevinsky, GA .

FEBS LETTERS, 1999, 455 (1-2) :154-158

[6] X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293) - An initial glance of the viral DNA binding platform [J].

Chen, ZG ;

Yan, YW ;

Munshi, S ;

Li, Y ;

Zugay-Murphy, J ;

Xu, B ;

Witmer, M ;

Felock, P ;

Wolfe, A ;

Sardana, V ;

Emini, EA ;

Hazuda, D ;

Kuo, LC .

JOURNAL OF MOLECULAR BIOLOGY, 2000, 296 (02) :521-533

[7] COSALANE ANALOGS WITH ENHANCED POTENCIES AS INHIBITORS OF HIV-1 PROTEASE AND INTEGRASE [J].

CUSHMAN, M ;

GOLEBIEWSKI, WM ;

POMMIER, Y ;

MAZUMDER, A ;

REYMEN, D ;

DECLERCQ, E ;

GRAHAM, L ;

RICE, WG .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (03) :443-452

[8] Identification of a nucleotide binding site in HTV-1 integrase [J].

Drake, RR ;

Neamati, N ;

Hong, HX ;

Pilon, AA ;

Sunthankar, P ;

Hume, SD ;

Milne, GWA ;

Pommier, Y .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1998, 95 (08) :4170-4175

[9] HIV integrase structure and function [J].

Esposito, D ;

Craigie, R .

ADVANCES IN VIRUS RESEARCH, VOL 52, 1999, 52 :319-333

[10] Sequence specificity of viral end DNA binding by HIV-1 integrase reveals critical regions for protein-DNA interaction [J].

Esposito, D ;

Craigie, R .

EMBO JOURNAL, 1998, 17 (19) :5832-5843

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