基础医学与临床 ›› 2017, Vol. 37 ›› Issue (4): 548-552.

• 短篇综述 • 上一篇    下一篇

G蛋白偶联受体激酶2活性和表达的调控及其在恶性肿瘤中的作用

徐周纬1,严尚学2,吴华勋2,陈镜宇2,张影2,魏伟2   

  1. 1. 安徽医科大学第一附属医院
    2. 安徽医科大学临床药理研究所
  • 收稿日期:2016-05-03 修回日期:2016-06-30 出版日期:2017-04-05 发布日期:2017-03-24
  • 通讯作者: 徐周纬 E-mail:xzw0318@sohu.com
  • 基金资助:
    国家自然科学基金面上项目;国家自然科学基金面上项目;安徽省自然科学基金面上项目

Regulation of activity and expression of GRK2 and its role in treatment of malignant tumors

  • Received:2016-05-03 Revised:2016-06-30 Online:2017-04-05 Published:2017-03-24
  • Contact: Zhou-Wei XU E-mail:xzw0318@sohu.com
  • Supported by:
    the National Natural Science Foundation of China;the National Natural Science Foundation of China

摘要: G蛋白偶联受体激酶2(GRK2)属于丝氨酸/苏氨酸蛋白激酶家族,广泛分布于各种组织中,能够特异性的使活化的G蛋白偶联受体(GPCRs)发生磷酸化及脱敏,从而终止GPCRs介导的信号转导通路。GRK2不仅能够调节GPCRs和非GPCRs,其自身活性和表达也可受到多种因素的调节。GRK2具有多种不同的生理及病理作用,其涉及的许多信号通路与恶性肿瘤的发生发展密切相关。

关键词: G蛋白偶联受体, G蛋白偶联受体激酶2, 活性调控, 表达调控, 恶性肿瘤

Abstract: G protein-coupled receptor kinases 2 (GRK2), which belongs to the serine/threonine protein kinase family, is widely distributed in a variety of tissues.With its specificity, it can enable activated G protein-coupled receptors (GPCRs) to be phosphorylated and desensitized, thus terminating the signal transduction pathways mediated by GPCRs.GRK2 can modulate GPCRs and non-GPCRs, but its own activity and expression may also be subject to the regulation of a number of factors. GRK2 has a variety of physiological and pathological effects, and many signaling pathways involved are closely related to the occurrence and development of malignant tumors.

Key words: G protein coupled receptors, G protein coupled receptor kinase 2, activity regulation, expression regulation, malignant tumor