Design and discovery of HIV-1 integrase inhibitors

被引：63

作者：

Neamati, N

Sunder, S

Pommier, Y

机构：

[1] Laboratory of Molecular Pharmacology, Division of Basic Sciences, Building 37, Bethesda

来源：

DRUG DISCOVERY TODAY | 1997年 / 2卷 / 11期

关键词：

D O I：

10.1016/S1359-6446(97)01105-7

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The rapid emergence of human immunodeficiency virus (HIV) strains resistant to available drugs implies that effective treatment modalities will require the use of a combination of drugs targeting different sites of the HIV life cycle. Integrase is emerging as a novel target for intervention by chemotherapeutics. As part of a program to develop novel antiviral agents, we have studied a large number of compounds with activity against HIV-1 replication in the National Cancer Institute (NCI) Antiviral Drug Program. In this review, we present a comprehensive review of all such inhibitors reported to date.

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收藏

页码：487 / 498

页数：12

相关论文

共 57 条

[1] ISOLATION OF HIGH-AFFINITY RNA LIGANDS TO HIV-1 INTEGRASE FROM A RANDOM POOL [J].

ALLEN, P ;

WORLAND, S ;

GOLD, L .

VIROLOGY, 1995, 209 (02) :327-336

[2]

[Anonymous], J PHARM MED

[3] Inhibition of human immunodeficiency virus type 1 integrase by the Fab fragment of a specific monoclonal antibody suggests that different multimerization states are required for different enzymatic functions [J].

Barsov, EV ;

Huber, WE ;

Marcotrigiano, J ;

Clark, PK ;

Clark, AD ;

Arnold, E ;

Hughes, SH .

JOURNAL OF VIROLOGY, 1996, 70 (07) :4484-4494

[4] HIV-1 INTEGRASE - HIGH-LEVEL PRODUCTION AND SCREENING ASSAY FOR THE ENDONUCLEOLYTIC ACTIVITY [J].

BILLICH, A ;

SCHAUER, M ;

FRANK, S ;

ROSENWIRTH, B ;

BILLICH, S .

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY, 1992, 3 (02) :113-119

[5] MONOCLONAL-ANTIBODIES AGAINST HIV TYPE-1 INTEGRASE - CLUES TO MOLECULAR-STRUCTURE [J].

BIZUBBENDER, D ;

KULKOSKY, J ;

SKALKA, AM .

AIDS RESEARCH AND HUMAN RETROVIRUSES, 1994, 10 (09) :1105-1115

[6] HIGH-RESOLUTION STRUCTURE OF THE CATALYTIC DOMAIN OF AVIAN-SARCOMA VIRUS INTEGRASE [J].

BUJACZ, G ;

JASKOLSKI, M ;

ALEXANDRATOS, J ;

WLODAWER, A ;

MERKEL, G ;

KATZ, RA ;

SKALKA, AM .

JOURNAL OF MOLECULAR BIOLOGY, 1995, 253 (02) :333-346

[7] HYDROXYLATED AROMATIC INHIBITORS OF HIV-1 INTEGRASE [J].

BURKE, TR ;

FESEN, MR ;

MAZUMDER, A ;

WANG, J ;

CAROTHERS, AM ;

GRUNBERGER, D ;

DRISCOLL, J ;

KOHN, K ;

POMMIER, Y .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (21) :4171-4178

[8] INHIBITION OF THE IN-VITRO INTEGRATION OF MOLONEY MURINE LEUKEMIA-VIRUS DNA BY THE DNA MINOR-GROOVE BINDER NETROPSIN [J].

CARTEAU, S ;

MOUSCADET, JF ;

GOULAOUIC, H ;

SUBRA, F ;

AUCLAIR, C .

BIOCHEMICAL PHARMACOLOGY, 1994, 47 (10) :1821-1826

[9] INHIBITORY EFFECT OF THE POLYANIONIC DRUG SURAMIN ON THE IN-VITRO HIV DNA INTEGRATION REACTION [J].

CARTEAU, S ;

MOUSCADET, JF ;

GOULAOUIC, H ;

SUBRA, F ;

AUCLAIR, C .

ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1993, 305 (02) :606-610

[10] EFFECT OF TOPOISOMERASE INHIBITORS ON THE INVITRO HIV DNA INTEGRATION REACTION [J].

CARTEAU, S ;

MOUSCADET, JF ;

GOULAOUIC, H ;

SUBRA, F ;

AUCLAIR, C .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1993, 192 (03) :1409-1414

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