自然杂志 ›› 2021, Vol. 43 ›› Issue (1): 18-24.doi: 10.3969/j.issn.0253-9608.2021.01.003

• 专题综述 • 上一篇    下一篇

趋化因子受体的结构与信号转导机制

刘凯雯,刘志杰,华甜   

  1. 上海科技大学 iHuman研究所,上海 201210 
  • 收稿日期:2021-10-01 出版日期:2021-02-25 发布日期:2021-02-25
  • 通讯作者: 刘志杰,通信作者,研究方向:结构生物学。 华甜,通信作者,研究方向:结构生物学。

Structural and signaling mechanism of chemokine receptors

LIU Kaiwen, LIU Zhijie, HUA Tian   

  1. iHuman Institute, ShanghaiTech University, Shanghai 201210, China
  • Received:2021-10-01 Online:2021-02-25 Published:2021-02-25

摘要: 趋化因子(chemokine)及趋化因子受体(chemokine receptor)在介导细胞迁移、增殖和抵御病原体入侵过程中发挥重要作用,并且与免疫环境中炎症和癌症的发生发展密切相关。人体中有20多种趋化因子受体和近50种趋化因子。一种趋化因子可以结合多种受体,反之亦然,它们相互作用构成了复杂的趋化因子调控网络。对趋化因子及其受体的三维结构的解析,对于我们更深入理解趋化因子受体家族的激活机制与药理功能具有非常重要的意义。文章总结了已解析的与内 源性趋化因子配体或其类似物结合的趋化因子受体结构,分析了趋化因子激活相应趋化因子受体的分子机制,以及对于抗 癌药物开发设计的重要性。

关键词:  , G蛋白偶联受体;趋化因子;趋化因子受体;激活机制;结构生物学

Abstract: Chemokine and chemokine receptor play important roles in cell migration, proliferation and resisting invasion, thus closely related with multiple fundamental biological processes and disease development in immune environment, such as inflammation and cancer. There are more than 20 different chemokine receptors and nearly 50 chemokines in human body. One chemokine can bind multiple receptors and vice versa. Their interaction forms a complex chemokine regulatory network. Analysis of the three-dimensional structures of chemokines and their receptors will further improve our understanding of the activation mechanism and pharmacological functions of the chemokine receptor family. Here, we briefly review the solved structure of chemokine receptors bound with chemokine ligands or their analogs, and analyze the structure and activation mechanism of chemokine receptors, and indicate the importance of the anticancer drug development of chemokine receptor family.