G蛋白偶联受体激酶活性调控及其在恶性肿瘤中的作用

Regulation of G protein-coupled receptor kinases activity and their role in malignant tumors

G蛋白偶联受体(GPCR),是一类重要的细胞表面受体。G蛋白偶联受体激酶(GRK)属于丝氨酸/苏氨酸蛋白激酶家族,其亚型广泛存在与各种组织,能够特异性地使活化的GPCR发生磷酸化及脱敏,从而终止GPCR介导的信号转导通路。新的研究还发现,GRK不仅作用于GPCR,也可以通过使非GPCR磷酸化或通过非磷酸化作用参与信号转导。GRK不仅能够调节GPCR和非GPCR,其自身活性也可受到多种因素的调节。本文结合GRK的多种功能作用和GRK活性调控,对GRK在脑、内分泌、生殖系统、消化系统及黑色素肿瘤中的作用做简要综述。

G protein coupled receptors（GPCR） are a superfamily of membrane sensors with the key roles in physiology and as pharmacological targets.G PCR kinases（GRK） constitute a family of seven serine/threonine protein kinases that specifically recognize and phosphorylate agonist-activated GPCR,thereby terminating the GPCR-mediated signal transduction pathway.Recently researches found that GRK also interact with non-GPCR or participate in signal transduction in non-phosphorylated manner.Besides,GRK activity is mediated by multiple factors.In this article,the function of GRK,the regulation of GRK activity and GRK-mediated functions in human cancers were reviewed.