趋化因子受体 CCR5 的小分子拮抗剂。

Small molecule antagonists of the chemokine receptor CCR5.

机构信息

Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304 USA.

出版信息

Curr Top Med Chem. 2010;10(13):1299-338. doi: 10.2174/156802610791561219.

PMID:20536424

Abstract

This review will focus on the discovery and clinical development of small molecule antagonists of CCR5 for the treatment of HIV-1/AIDS, as well as for the potential treatment of inflammatory diseases. In particular, we will focus on the specific medicinal chemistry problems that were faced during the discovery of the molecules. We will also describe limited data from clinical development phases focusing on specific issues that arose during the clinical trials. Finally, we will touch on the mechanism of action of CCR5 antagonists.

摘要

本篇综述聚焦于 CCR5 小分子拮抗剂的发现和临床开发，以用于治疗 HIV-1/AIDS，以及用于治疗炎症性疾病。特别是，我们将重点介绍在发现这些分子过程中所面临的特定药物化学问题。我们还将描述临床开发阶段的有限数据，重点介绍临床试验中出现的具体问题。最后，我们将探讨 CCR5 拮抗剂的作用机制。