Crucial amides for dimerization inhibitors of HIV-1 protease

被引:10
|
作者
Bowman, MJ [1 ]
Chmielewski, J [1 ]
机构
[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
基金
美国国家卫生研究院;
关键词
D O I
10.1016/j.bmcl.2003.09.099
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An inhibitor based on crosslinked peptides from the interfacial region of HIV-1 protease, previously shown to act by dimerization inhibition, was modified by N-methylation to ascertain the importance of the amide hydrogens on inhibition. The effects of N-methylation on HIV-1 protease inhibition, as well as the effects on degradation by proteases are described. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1395 / 1398
页数:4
相关论文
共 50 条
  • [31] HIV-1 protease and its inhibitors
    Geller, M
    Trylska, J
    Antosiewicz, J
    THEORETICAL AND COMPUTATIONAL METHODS IN GENOME RESEARCH, 1997, : 237 - 254
  • [32] AZIRIDINE INHIBITORS OF HIV-1 PROTEASE
    LEVERETT, B
    BAI, JC
    POST, CB
    LOUDON, GM
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1994, 208 : 37 - MEDI
  • [33] HIV-1 protease inhibitors and mechanisms of HIV-1's resistance
    Das, Debananda
    GLOBAL HEALTH & MEDICINE, 2024, 6 (06): : 357 - 362
  • [34] Peptidomimetic dimerization inhibitors of HIV-1 protease:: Further insights into structural variations and mechanism of action
    Bannwarth, Ludovic
    Rose, Thierry
    Frutos, Silvia
    Giralt, Ernest
    Vanderesse, Regis
    Jamart-Gregoire, Brigitte
    Vidu, Anamaria
    Ongeri, Sandrine
    Sicsic, Sames
    Pannecouque, Christophe
    De Clercq, Erik
    Reboud-Ravaux, Michele
    ANTIVIRAL RESEARCH, 2007, 74 (03) : A64 - A64
  • [35] Design, synthesis, and evaluation of conformationally constrained tongs, new inhibitors of HIV-1 protease dimerization
    Bouras, A
    Boggetto, N
    Benatalah, Z
    de Rosny, E
    Sicsic, S
    Reboud-Ravaux, M
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (06) : 957 - 962
  • [36] Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase:: A single mode of inhibition for the three HIV enzymes?
    Camarasa, Maria-Jose
    Velazquez, Sonsoles
    San-Felix, Ana
    Perez-Perez, Maria-Jesus
    Gago, Federico
    ANTIVIRAL RESEARCH, 2006, 71 (2-3) : 260 - 267
  • [37] A GENERAL STRATEGY TOWARDS THE DIMERIZATION INHIBITION OF HIV-1 PROTEASE
    ZUTSHI, R
    BISHOP, P
    CHMIELEWSKI, J
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1995, 210 : 347 - ORGN
  • [38] How Does Darunavir Prevent HIV-1 Protease Dimerization?
    Huang, Danzhi
    Caflisch, Amedeo
    JOURNAL OF CHEMICAL THEORY AND COMPUTATION, 2012, 8 (05) : 1786 - 1794
  • [39] NOVEL PSEUDOSYMMETRIC INHIBITORS OF HIV-1 PROTEASE
    FASSLER, A
    ROSEL, J
    GRUTTER, M
    TINTELNOTBLOMLEY, M
    ALTERI, E
    BOLD, G
    LANG, M
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (12) : 2837 - 2842
  • [40] Switching between allosteric and dimerization inhibition of HIV-1 protease
    Bowman, MJ
    Byrne, S
    Chmielewski, J
    CHEMISTRY & BIOLOGY, 2005, 12 (04): : 439 - 444