The role of 2′,3′-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V)

被引：11

作者：

Choo, H ^{[1
]}

Chong, YH ^{[1
]}

Chu, CK ^{[1
]}

机构：

[1] Univ Georgia, Coll Pharm, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(03)00330-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Molecular modeling studies show that the 2',3-double bond of the sugar moiety of various 2', 3'-unsaturated nucleosides interacts with the aromatic moiety of Tyr115 of HIV-1 reverse transcriptase (RT) by hydrophobic pi-pi interaction. In 3TC-resistant mutant (M184V) RT, 2'-fluoro-2,3-unsaturated nucleosides with a bulky 4-substituent experience significant steric hindrance with the side chain of Val184. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1993 / 1996

页数：4

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