Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors

被引：112

作者：

Kazmierski, W

Bifulco, N

Yang, HB

Boone, L

DeAnda, F

Watson, C

Kenakin, T

机构：

[1] GlaxoSmithKline Res & Dev Ltd, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline Res & Dev Ltd, Dept Virol, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline Res & Dev Ltd, Computat Analyt & Struct Sci, Res Triangle Pk, NC 27709 USA

[4] GlaxoSmithKline Res & Dev Ltd, Syst Res, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 13期

关键词：

D O I：

10.1016/S0968-0896(03)00161-5

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：

This review addresses key pharmacology and virology issues relevant in discovery and development of CCR5 antagonists as anti-HIV drugs, such as target validation, receptor internalization, allosterism, viral resistance and tropism. Recent progress in the discovery and development of CCR5 antagonists, SAR and clinical status are reviewed. Finally, modeling-based structure of CCR5 is discussed in the context of a small-molecule antagonism of the CCR5 receptor. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：2663 / 2676

页数：14

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