The active site of HIV-1 protease

被引：26

作者：

Mager, PP ^{[1
]}

机构：

[1] Univ Leipzig, Inst Pharmacol & Toxicol, Res Grp Pharmacochem, D-04107 Leipzig, Saxony, Germany

来源：

MEDICINAL RESEARCH REVIEWS | 2001年 / 21卷 / 04期

关键词：

medicinal chemistry; molecular simulation; molecular modeling; HIV-1; protease;

D O I：

10.1002/med.1012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The active site of the homodimeric HIV-1 protease includes six amino acids (triads AspThrGly found in each monomer) in amino acid positions 25 to 27 and 25 ' to 27 '. Up to now, the role of Thr26 and Thr26 ', and Gly27 and Gly27 ', is unknown. It is hypothesized that strong hydrogen-bonding forces between the Thr26 and Thr26 ' residues stabilize the conformational state of the active site, and that the function of Gly27 and Gly27 ' is to accommodate and bind a substrate in a position in which the catalytic Asp25 and Asp25 ' carboxylate groups can attack the amide moiety of a substrate. (C) 2001 John Wiley & Sons, Inc.

引用

页码：348 / 353

页数：6

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