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
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
收藏
页码:139 / 148
页数:10
相关论文
共 57 条
[51]   Solution structure of anti-HIV-1 and anti-tumor protein MAP30: Structural insights into its multiple functions [J].
Wang, YX ;
Neamati, N ;
Jacob, J ;
Palmer, I ;
Stahl, SJ ;
Kaufman, JD ;
Huang, PL ;
Huang, PL ;
Winslow, HE ;
Pommier, Y ;
Wingfield, PT ;
Lee-Huang, S ;
Bax, A ;
Torchia, DA .
CELL, 1999, 99 (04) :433-442
[52]   Recognition of the four Watson-Crick base pairs in the DNA minor groove by synthetic ligands [J].
White, S ;
Szewczyk, JW ;
Turner, JM ;
Baird, EE ;
Dervan, PB .
NATURE, 1998, 391 (6666) :468-471
[53]   Crystal structures of catalytic core domains of retroviral integrases and role of divalent cations in enzymatic activity [J].
Wlodawer, A .
ADVANCES IN VIRUS RESEARCH, VOL 52, 1999, 52 :335-U15
[54]   Crystal structure of an active two-domain derivative of Rous sarcoma virus integrase [J].
Yang, ZN ;
Mueser, TC ;
Bushman, FD ;
Hyde, CC .
JOURNAL OF MOLECULAR BIOLOGY, 2000, 296 (02) :535-548
[55]   Inhibition of HIV integrase by novel nucleotides bearing tricyclic bases [J].
Zhang, JZ ;
Neamati, N ;
Pommier, Y ;
Nair, V .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (14) :1887-1890
[56]   Irreversible inhibition of human immunodeficiency virus type 1 integrase by dicaffeoylquinic acids [J].
Zhu, K ;
Cordeiro, ML ;
Atienza, J ;
Robinson, WE ;
Chow, SA .
JOURNAL OF VIROLOGY, 1999, 73 (04) :3309-3316
[57]   Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture [J].
Zouhiri, F ;
Mouscadet, JF ;
Mekouar, K ;
Desmaële, D ;
Savouré, D ;
Leh, H ;
Subra, F ;
Le Bret, M ;
Auclair, C ;
d'Angelo, J .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (08) :1533-1540