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

被引:85
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
  • [1] SYNTHETIC NON-PEPTIDE INHIBITORS OF HIV PROTEASE
    BLUMENSTEIN, JJ
    COPELAND, TD
    OROSZLAN, S
    MICHEJDA, CJ
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 163 (02) : 980 - 987
  • [2] 18TH KREBS,HANS LECTURE - KNOWLEDGE-BASED PROTEIN MODELING AND DESIGN
    BLUNDELL, T
    CARNEY, D
    GARDNER, S
    HAYES, F
    HOWLIN, B
    HUBBARD, T
    OVERINGTON, J
    SINGH, DA
    SIBANDA, BL
    SUTCLIFFE, M
    [J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1988, 172 (03): : 513 - 520
  • [3] RETROVIRAL PROTEINASES - A 2ND FRONT AGAINST AIDS
    BLUNDELL, T
    PEARL, L
    [J]. NATURE, 1989, 337 (6208) : 596 - 597
  • [4] ON THE RATIONAL DESIGN OF RENIN INHIBITORS - X-RAY STUDIES OF ASPARTIC PROTEINASES COMPLEXED WITH TRANSITION-STATE ANALOGS
    BLUNDELL, TL
    COOPER, J
    FOUNDLING, SI
    JONES, DM
    ATRASH, B
    SZELKE, M
    [J]. BIOCHEMISTRY, 1987, 26 (18) : 5585 - 5590
  • [5] X-RAY ANALYSES OF ASPARTIC PROTEINASES - THE 3-DIMENSIONAL STRUCTURE AT 2.1 A RESOLUTION OF ENDOTHIAPEPSIN
    BLUNDELL, TL
    JENKINS, JA
    SEWELL, BT
    PEARL, LH
    COOPER, JB
    TICKLE, IJ
    VEERAPANDIAN, B
    WOOD, SP
    [J]. JOURNAL OF MOLECULAR BIOLOGY, 1990, 211 (04) : 919 - 941
  • [6] 3-DIMENSIONAL STRUCTURE OF THE COMPLEX OF THE RHIZOPUS-CHINENSIS CARBOXYL PROTEINASE AND PEPSTATIN AT 2.5-A RESOLUTION
    BOTT, R
    SUBRAMANIAN, E
    DAVIES, DR
    [J]. BIOCHEMISTRY, 1982, 21 (26) : 6956 - 6962
  • [7] CRYSTALLIZABLE HIV-1 PROTEASE DERIVED FROM EXPRESSION OF THE VIRAL POL GENE IN ESCHERICHIA-COLI
    DANLEY, DE
    GEOGHEGAN, KF
    SCHELD, KG
    LEE, SE
    MERSON, JR
    HAWRYLIK, SJ
    RICKETT, GA
    AMMIRATI, MJ
    HOBART, PM
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 165 (03) : 1043 - 1050
  • [8] INHIBITION OF HUMAN IMMUNODEFICIENCY VIRUS-1 PROTEASE INVITRO - RATIONAL DESIGN OF SUBSTRATE-ANALOG INHIBITORS
    DREYER, GB
    METCALF, BW
    TOMASZEK, TA
    CARR, TJ
    CHANDLER, AC
    HYLAND, L
    FAKHOURY, SA
    MAGAARD, VW
    MOORE, ML
    STRICKLER, JE
    DEBOUCK, C
    MEEK, TD
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (24) : 9752 - 9756
  • [9] DESIGN, ACTIVITY, AND 2.8 A CRYSTAL-STRUCTURE OF A C2 SYMMETRICAL INHIBITOR COMPLEXED TO HIV-1 PROTEASE
    ERICKSON, J
    NEIDHART, DJ
    VANDRIE, J
    KEMPF, DJ
    WANG, XC
    NORBECK, DW
    PLATTNER, JJ
    RITTENHOUSE, JW
    TURON, M
    WIDEBURG, N
    KOHLBRENNER, WE
    SIMMER, R
    HELFRICH, R
    PAUL, DA
    KNIGGE, M
    [J]. SCIENCE, 1990, 249 (4968) : 527 - 533
  • [10] EXPRESSION AND PROCESSING OF THE AIDS VIRUS REVERSE-TRANSCRIPTASE IN ESCHERICHIA-COLI
    FARMERIE, WG
    LOEB, DD
    CASAVANT, NC
    HUTCHISON, CA
    EDGELL, MH
    SWANSTROM, R
    [J]. SCIENCE, 1987, 236 (4799) : 305 - 308