CCR1 antagonists

被引:37
作者
Cheng, Jie-Fei [1 ]
Jack, Rick [1 ]
机构
[1] Tanabe Res Labs USA Inc, San Diego, CA 92121 USA
关键词
chemokines; CCR1; G protein-coupled receptors; MIP-1; alpha; RANTES; receptor antagonists; GPCR;
D O I
10.1007/s11030-008-9076-x
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
CCR1 (CC Chemokine receptor 1) is a widely studied G protein-coupled receptor target expressed on multiple types of leukocytes. It is implicated in initiating and exacerbating inflammatory conditions and thus is viewed as a good target for autoimmune and inflammatory therapeutic applications. Numerous CCR1 antagonists have been reported. Although some early CCR1 antagonists lacked the species cross reactivity that made in vivo animal model study difficult, efforts have been made to improve the compound potency in rodents. Recent identification of new and improved CCR1 antagonists has resulted in promising, in vivo efficacy in a variety of animal models of disease. While several early compounds have been withdrawn from clinical trials due to lack of efficacy, work continues to evaluate CCR1 antagonists in preclinical and clinical settings.
引用
收藏
页码:17 / 23
页数:7
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