CCR5拮抗剂新药理作用及机制研究进展  

Advances in new indications and their mechanisms of CCR5 antagonists

作　　者：郑玉贵 陈欢[2,3] 罗荣华 郑昌博[1] ZHENG Yu-gui;CHEN Huan;LUO Rong-hua;ZHENG Chang-bo(School of Pharmaceutical Science&Yunnan Key Lab of Pharmacology for Natural Products,Kunming Medical University,Kunming 650500,China;Key Lab of Bioactive Peptides of Yunnan Province/Key Lab of Animal Models and Human Disease Mechanisms of Chinese Academy of Science,Kunming Institute of Zoology,Chinese Academy of Sciences,Kunming 650223,China;Key Lab of Molecular Biology for Sinomedicine,Yunnan University of Chinese Medicine,Kunming 650500,China)

机构地区：[1]昆明医科大学,药学院暨云南省天然药物药理重点实验室,云南昆明650500 [2]中国科学院昆明动物研究所,云南省活性多肽研究与利用重点实验室/中国科学院动物模型与人类疾病机理重点实验室,云南昆明650223 [3]云南中医药大学中医药学分子生物学重点实验室,云南昆明650500

出　　处：《中国药理学通报》2020年第6期763-767,共5页Chinese Pharmacological Bulletin

基　　金：中国科学院个性化药物先导专项课题(No XDA12020227);国家科技重大专项“十三五”计划课题(No 2018ZX09711002-014-007);云南省活性多肽研究与利用重点实验室开放课题(No AMHD-2017-3);云南省教育厅科学研究基金项目(No 2018JS163)。

摘　　要：C-C趋化因子受体5(C-C chemokine receptor 5,CCR5)是G蛋白偶联受体家族成员,在多种细胞表面表达,CCR5与其特异性配体结合而发挥生物学作用。随着对CCR5蛋白的深入研究发现,CCR5作为辅助受体不仅介导HIV的感染过程,还参与许多疾病的病理过程。因此,CCR5拮抗剂非抗HIV药理作用不断被发现,其抗肿瘤、抗炎、抗排异等活性作用的研究逐渐增多,拓宽了其临床适应症。本文简要综述了CCR5拮抗剂的新发现药理作用及机制研究进展,以期为CCR5拮抗剂的进一步研究和开发提供参考。Chemokine receptor 5(CCR5)belongs to a G protein-coupled receptors family which is expressed on a variety of cells and binds to its specific ligands to play a biological role.With the in-depth study of CCR5,CCR5 not only participates in the HIV infection process as co-receptor,but also mediates other physiological and pathological processes.Therefore,the non-anti-HIV pharmacological function of CCR5 antagonists has been continuously discovered,and the study of its anti-tumor,anti-inflammatory and anti-rejection activities has gradually increased,expanding its clinical indications.Here we review the related biological functions of CCR5,the newly discovered indications and mechanisms of CCR5 antagonists,hoping to provide reference for further research and development of CCR5 antagonists.

关 键 词：CCR5拮抗剂 抗肿瘤 抗炎症反应 抗微生物 新适应症 临床试验 

分 类 号：R05[医药卫生] R341