趋化因子受体拮抗剂：第二部分。
Chemokine receptor antagonists: part 2.
作者信息
Pease James E, Horuk Richard
机构信息
Faculty of Medicine National Heart and Lung Institute, Imperial College of Science, Technology & Medicine, Leukocyte Biology Section, London, UK.
出版信息
Expert Opin Ther Pat. 2009 Feb;19(2):199-221. doi: 10.1517/13543770802641353.
BACKGROUND
The first part of this two-part review discussed approaches to generating antagonists for some of the CC chemokine receptors, including CCR1, CCR2, CCR3, and CCR4.
OBJECTIVE/METHOD: This second part of the series concludes the review by describing antagonists for CCR5, CCR8, CCR9, CXCR3, CXCR4, and promiscuous antagonists.
CONCLUSION
Chemokine receptor antagonists have found mixed success as therapeutics. Although one antagonist--maraviroc, a CCR5 inhibitor to treat AIDS--has been registered as an approved drug, this is the only success so far. There have been many failures in the clinic and we discuss the idea of promiscuous receptor antagonists as an alternative approach.
背景
在这个分两部分的综述的第一部分中，我们讨论了针对一些CC趋化因子受体（包括CCR1、CCR2、CCR3和CCR4）生成拮抗剂的方法。
目的/方法：本系列的第二部分通过描述CCR5、CCR8、CCR9、CXCR3、CXCR4的拮抗剂以及通用型拮抗剂来完成本综述。
结论
趋化因子受体拮抗剂作为治疗药物的效果喜忧参半。尽管有一种拮抗剂——马拉维若，一种用于治疗艾滋病的CCR5抑制剂——已作为获批药物上市，但这是目前唯一成功的案例。临床上有许多失败的案例，我们讨论了通用型受体拮抗剂作为一种替代方法的设想。
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