The role of G protein-coupled receptor kinases in the pathology of malignant tumors

被引：20
作者：
Sun, Wu-yi [1 ]
Wu, Jing-jing [1 ,2 ]
Peng, Wen-ting [1 ]
Sun, Jia-chang [1 ]
Wei, Wei [1 ]
机构：
[1] Anhui Med Univ, Key Lab Antiinflammatory & Immune Med, Minist Educ, Inst Clin Pharmacol, Hefei 230032, Anhui, Peoples R China
[2] Anhui Med Univ, Affiliated Hosp 2, Dept Oncol, Hefei 230601, Anhui, Peoples R China
来源：
ACTA PHARMACOLOGICA SINICA | 2018年 / 39卷 / 11期
基金：
中国国家自然科学基金;
关键词：
G protein-coupled receptors; G protein coupling receptor kinases; Breast cancer; Prostate cancer; Hepatocellular carcinoma; Lung cancer; HEPATOCELLULAR-CARCINOMA CELLS; NEGATIVE BREAST-CANCER; 2; GRK2; PROSTATE-CANCER; HEPG2; CELLS; C-SRC; EXPRESSION; GROWTH; PHOSPHORYLATION; BETA;
D O I：
10.1038/s41401-018-0049-z
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
G protein-coupled receptor kinases (GRKs) constitute seven subtypes of serine/threonine protein kinases that specifically recognize and phosphorylate agonist-activated G protein-coupled receptors (GPCRs), thereby terminating the GPCRs-mediated signal transduction pathway. Recent research shows that GRKs also interact with non-GPCRs and participate in signal transduction in non-phosphorylated manner. Besides, GRKs activity can be regulated by multiple factors. Changes in GRKs expression have featured prominently in various tumor pathologies, and they are associated with angiogenesis, proliferation, migration, and invasion of malignant tumors. As a result, GRKs have been intensively studied as potential therapeutic targets. Herein, we review evolving understanding of the function of GRKs, the regulation of GRKs activity and the role of GRKs in human malignant tumor pathophysiology.
引用
收藏
页码：1699 / 1705
页数：7
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