THE 3-D STRUCTURE OF HIV-1 PROTEINASE AND THE DESIGN OF ANTIVIRAL AGENTS FOR THE TREATMENT OF AIDS

被引:86
作者
BLUNDELL, TL
LAPATTO, R
WILDERSPIN, AF
HEMMINGS, AM
HOBART, PM
DANLEY, DE
WHITTLE, PJ
机构
[1] PFIZER INC,GROTON,CT 06340
[2] PFIZER LTD,SANDWICH CT13 9NJ,KENT,ENGLAND
关键词
D O I
10.1016/0968-0004(90)90280-O
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A proteinase is essential for replication of HIV. Cloning and chemical synthesis have provided a sufficient supply of HIV-1 proteinase for the determination of its three-dimensional structure. Analogies between the structures of HIV-1 proteinase and the mammalian enzyme renin, which is involved in the control of blood pressure, have given important clues concerning the design of specific inhibitors that have antiviral activity. © 1990.
引用
收藏
页码:425 / 430
页数:6
相关论文
共 39 条
[21]   STRUCTURE OF COMPLEX OF SYNTHETIC HIV-1 PROTEASE WITH A SUBSTRATE-BASED INHIBITOR AT 2.3-A RESOLUTION [J].
MILLER, M ;
SCHNEIDER, J ;
SATHYANARAYANA, BK ;
TOTH, MV ;
MARSHALL, GR ;
CLAWSON, L ;
SELK, L ;
KENT, SBH ;
WLODAWER, A .
SCIENCE, 1989, 246 (4934) :1149-1152
[22]   CRYSTAL-STRUCTURE OF A RETROVIRAL PROTEASE PROVES RELATIONSHIP TO ASPARTIC PROTEASE FAMILY [J].
MILLER, M ;
JASKOLSKI, M ;
RAO, JKM ;
LEIS, J ;
WLODAWER, A .
NATURE, 1989, 337 (6207) :576-579
[23]   3-DIMENSIONAL STRUCTURE OF ASPARTYL PROTEASE FROM HUMAN IMMUNODEFICIENCY VIRUS HIV-1 [J].
NAVIA, MA ;
FITZGERALD, PMD ;
MCKEEVER, BM ;
LEU, CT ;
HEIMBACH, JC ;
HERBER, WK ;
SIGAL, IS ;
DARKE, PL ;
SPRINGER, JP .
NATURE, 1989, 337 (6208) :615-620
[24]  
NOELLING K, 1990, FEBS LETT, V261, P373
[25]   THE ACTIVE-SITE OF ASPARTIC PROTEINASES [J].
PEARL, L ;
BLUNDELL, T .
FEBS LETTERS, 1984, 174 (01) :96-101
[26]   A STRUCTURAL MODEL FOR THE RETROVIRAL PROTEASES [J].
PEARL, LH ;
TAYLOR, WR .
NATURE, 1987, 329 (6137) :351-354
[27]  
PEARL LH, 1990, RETROVIRAL PROTEASES
[28]   ROLE OF HUMAN IMMUNODEFICIENCY VIRUS TYPE-1-SPECIFIC PROTEASE IN CORE PROTEIN MATURATION AND VIRAL INFECTIVITY [J].
PENG, C ;
HO, BK ;
CHANG, TW ;
CHANG, NT .
JOURNAL OF VIROLOGY, 1989, 63 (06) :2550-2556
[29]   MOLECULAR-BIOLOGY OF HIV [J].
PETERLIN, BM ;
LUCIW, PA .
AIDS, 1988, 2 :S29-S40
[30]   HYDROXYETHYLAMINE ANALOGS OF THE P17/P24 SUBSTRATE CLEAVAGE SITE ARE TIGHT-BINDING INHIBITORS OF HIV PROTEASE [J].
RICH, DH ;
GREEN, J ;
TOTH, MV ;
MARSHALL, GR ;
KENT, SBH .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1285-1288