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细胞表面趋化因子受体2(CCR2)属于G蛋白偶联受体(GPCR)超家族成员,并且是单核细胞趋化蛋白1～4(MCP1～4)的受体。MCP 1～4是促炎症反应的化学诱导物,CCR2和MCP-1在人类侵蚀性疾病模型如动脉粥状硬化、多发性硬化症中均起显著作用。大量研究证明CCR2和MCP-1拮抗剂可以减少临床炎症模型的发病率,这些化学拮抗剂的结构多样,主要包括γ-氨基丁酰胺类、甘胺酰胺类、噻唑类、吲哚类、二取代双哌啶醇类、季铵盐类和不饱和杂环类等,它们表现出不同的药理活性。CCR2拮抗剂对各种与趋化因子相关的疾病具有较好的疗效,部分药物已经进入临床试验阶段,综述CCR2及其受体拮抗剂的研究进展。
Cell surface chemokine receptor 2 (CCR2) is a member of the G-protein coupled receptor (GPCR) superfamily and is a receptor for monocyte chemotactic protein 1-4 (MCP1-4). MCP 1 to 4 are chemical inducers of proinflammatory responses, and CCR2 and MCP-1 play significant roles in human aggressive disease models such as atherosclerosis and multiple sclerosis. Numerous studies have demonstrated that CCR2 and MCP-1 antagonists can reduce the incidence of clinical inflammatory models. These chemical antagonists have diverse structures, including gamma-aminobutylamides, glycosamides, thiazoles, indoles, disubstituted Piperidinols, quaternary ammonium salts and unsaturated heterocycles, etc., which exhibit different pharmacological activities. CCR2 antagonists have good curative effect on various chemokine-related diseases. Some drugs have entered the clinical trial phase. The research progress of CCR2 and its receptor antagonists is reviewed.