CCR5及其拮抗剂的研究进展

Recent Research on CCR5 and Its Antagonists

趋化因子CCR5,作为G蛋白偶联因子超家族(GPCR)成员的细胞膜蛋白,是HIV-1入侵机体细胞的主要辅助受体之一。以CCR5为靶点的HIV-1受体拮抗剂越来越受关注,主要有趋化因子衍生物、非肽类小分子化合物、单克隆抗体、肽类化合物等4类。这些抗病毒活性强、高亲和力的CCR5拮抗剂,已有一部分进入了临床试验阶段。就近年来CCR5拮抗剂的相关研究进展进行了综述。

Chemokine receptor 5 （CCR5）, as a member of the G protein-coupled receptor （GPCR） superfamily, is a membrane protein on cell surface and one of the major of coreceptors for HIV-1 infection. CCR5 has became a molecular target for the novel drugs against HIV-1, and antagonists for CCR5 could be grouped as following, chemokine derivatives, small molecule non-peptide compounds, molecular antibodies and peptides. These compounds with high anti-viral activity and affinity are at different stages, and some have been under clinical studies. Therefore, the development research in the different kind of CCR5 antagonists is reviewed.