C–C chemokine receptor 5(CCR5) is a cell membrane protein from G protein-coupled receptors (GPCR) family, which is an important modulator for leukocyte activation and mobilization. In the 1980s, several reports suggest that lack of the HIV-1 co-receptor, the chemokine receptor CCR5, offers protection against HIV infection. Later, it was shown that CCR5 was confirmed to be the most common co-receptor for the HIV-1 virus R5 strain. In recent years, many studies have shown that CCR5 is closely related to the development of various cancers and inflammations to facilitate the discovery of CCR5 antagonists. There are many types of CCR5 antagonists, mainly including chemokine derivatives, non-peptide small molecule compounds, monoclonal antibodies, and peptide compounds. This review focus on the recent research processes and pharmacological effects of CCR5 antagonists such as Maraviroc, TAK-779 and PRO 140. After focusing on the therapeutic effect of CCR5 antagonists on AIDS, it also discusses the therapeutic prospect of CCR5 in other diseases such as inflammation and tumor.

C–C趋化因子受体5（CCR5）是G蛋白偶联受体（GPCR）家族的细胞膜蛋白，它是白细胞激活和动员的重要调节剂。在1980年代，几份报告表明，缺乏HIV-1共同受体趋化因子受体CCR5可以抵抗HIV感染。后来，证实了CCR5被证实是HIV-1病毒R5株最常见的共受体。近年来，许多研究表明，CCR5与各种癌症和炎症的发生密切相关，以促进CCR5拮抗剂的发现。CCR5拮抗剂的类型很多，主要包括趋化因子衍生物，非肽小分子化合物，单克隆抗体和肽化合物。