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趋化因子受体5(CCR5)属于G蛋白偶联受体超家族,是HIV感染早期介导病毒进入机体的主要辅助受体。CCR5拮抗剂已经成为一类重要的抗HIV病毒药物,主要包括趋化因子衍生物、非肽类小分子化合物、单克隆抗体、肽类化合物等4类。目前,全世界各大医药公司和研究机构纷纷研发了许多高选择性、活性强、生物利用度高的非肽类小分子CCR5拮抗剂,其中Maraviroc在2007年被FDA批准上市,还有一些目前已经进入临床试验阶段。文中对1999年到2009年10年间文献报道的相关非肽类小分子CCR5拮抗剂进行了综述。
Chemokine receptor 5 (CCR5), a member of the G protein-coupled receptor superfamily, is a major ancillary receptor that mediates viral entry into the body early in HIV infection. CCR5 antagonists have become a class of important anti-HIV drugs, including chemokine derivatives, non-peptide small molecule compounds, monoclonal antibodies, peptides and other four categories. Currently, the world’s major pharmaceutical companies and research institutions have developed many high selectivity, activity, bioavailability of non-peptide small molecule CCR5 antagonists, including Maraviroc in 2007 FDA approved the listing, there are still some Has entered the clinical trial phase. In this paper, the related non-peptide small molecule CCR5 antagonists reported in the literature from 1999 to 2009 were reviewed.