PRELIMINARY STRUCTURAL-ANALYSIS OF THE MUTATIONS SELECTED BY NONNUCLEOSIDE INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE

被引:13
|
作者
TONG, L
CARDOZO, M
JONES, PJ
ADAMS, J
机构
[1] BOEHRINGER INGELHEIM PHARMACEUT INC,DEPT MED CHEM,900 RIDGEBURY RD,RIDGEFIELD,CT 06877
[2] BOEHRINGER INGELHEIM PHARMACEUT INC,DEPT ANALYT SCI,RIDGEFIELD,CT 06877
关键词
D O I
10.1016/S0960-894X(01)81262-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The crystal structure of HIV reverse transcriptase complexed with nevirapine showed that most of the mutations that confer resistance to non-nucleoside inhibitors of RT are clustered around the nevirapine binding pocket. Establishment of favorable interactions with conserved residues in this pocket is essential for the design of second generation RT inhibitors.
引用
收藏
页码:721 / 726
页数:6
相关论文
共 50 条
  • [1] MECHANISM OF INHIBITION OF HIV-1 REVERSE-TRANSCRIPTASE BY NONNUCLEOSIDE INHIBITORS
    ESNOUF, R
    REN, JS
    ROSS, C
    JONES, Y
    STAMMERS, D
    STUART, D
    [J]. NATURE STRUCTURAL BIOLOGY, 1995, 2 (04): : 303 - 308
  • [2] MECHANISM OF INHIBITION OF HIV-1 REVERSE-TRANSCRIPTASE BY NONNUCLEOSIDE INHIBITORS
    SPENCE, RA
    KATI, WM
    ANDERSON, KS
    JOHNSON, KA
    [J]. SCIENCE, 1995, 267 (5200) : 988 - 993
  • [3] MOLECULAR MODELING STUDIES OF HIV-1 REVERSE-TRANSCRIPTASE NONNUCLEOSIDE INHIBITORS
    KOEPKE, MBK
    ROUZER, CA
    TANEYHILL, LA
    SMITH, NA
    HUGHES, SH
    BOYER, PL
    ARNOLD, E
    DING, JP
    DAS, K
    TANTILLO, C
    KZHANG, WY
    MICHEJDA, CJ
    SMITH, RH
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1995, 210 : 93 - MEDI
  • [4] NONNUCLEOSIDE INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE - NEVIRAPINE AS A PROTOTYPE DRUG
    GROB, PM
    WU, JC
    COHEN, KA
    INGRAHAM, RH
    SHIH, CK
    HARGRAVE, KD
    MCTAGUE, TL
    MERLUZZI, VJ
    [J]. AIDS RESEARCH AND HUMAN RETROVIRUSES, 1992, 8 (02) : 145 - 152
  • [5] PREVENTION OF THE SPREAD OF HIV-1 INFECTION WITH NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS
    VASUDEVACHARI, MB
    BATTISTA, C
    LANE, HC
    PSALLIDOPOULOS, MC
    ZHAO, B
    COOK, J
    PALMER, JR
    ROMERO, DL
    TARPLEY, WG
    SALZMAN, NP
    [J]. VIROLOGY, 1992, 190 (01) : 269 - 277
  • [6] HIV-1 REVERSE-TRANSCRIPTASE RESIDUES THAT INFLUENCE SENSITIVITY TO NONNUCLEOSIDE INHIBITORS
    BYRNES, VW
    SARDANA, VV
    CONDRA, JH
    SCHLEIF, WA
    SCHNEIDER, CL
    WATERBURY, JA
    WOLFGANG, JA
    GRAHAM, DJ
    GOTLIB, L
    SCHLABACH, AJ
    WOLANSKI, BS
    LONG, WJ
    RHODES, A
    TITUS, DL
    ROTH, E
    BLAHY, OM
    EMINI, EA
    [J]. JOURNAL OF CELLULAR BIOCHEMISTRY, 1993, : 75 - 75
  • [7] DISCOVERY OF BISHETEROARYLPIPERAZINES (BHAP) AS NONNUCLEOSIDE HIV-1 REVERSE-TRANSCRIPTASE INHIBITORS
    ROMERO, DL
    PALMER, JR
    BUSSO, M
    REUSSER, F
    ARISTOFF, PA
    TAN, CK
    DOWNEY, K
    SO, A
    RESNICK, L
    TARPLEY, WG
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1990, 200 : 81 - MEDI
  • [8] THE GENETIC AND FUNCTIONAL BASIS OF HIV-1 RESISTANCE TO NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS
    EMINI, EA
    BYRNES, VW
    CONDRA, JH
    SCHLEIF, WA
    SARDANA, VV
    [J]. ARCHIVES OF VIROLOGY, 1994, : 11 - 17
  • [9] MODELING AND CLASSIFICATION OF CHEMICALLY UNRELATED HIV-1 NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS
    GUSSIO, R
    PATTABIRAMAN, N
    ZAHAREVITZ, DW
    KELLOGG, GE
    BURT, SK
    ERICKSON, JW
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1995, 209 : 107 - MEDI
  • [10] INHIBITION OF HIV-1 REPLICATION BY A NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITOR
    KOUP, RA
    HARGRAVE, K
    MERLUZZI, J
    ADAMS, J
    GROZINGER, K
    ECKNER, RJ
    SULLIVAN, JL
    [J]. JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES AND HUMAN RETROVIROLOGY, 1991, 4 (03): : 317 - 317