Review Article

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

Authors: Wu-yi Sun1, Jing-jing Wu1,2, Wen-ting Peng1, Jia-chang Sun1, Wei Wei1
1 Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of Antiinflammatory and Immune Medicine, Ministry of Education, Hefei 230032, China
2 Department of Oncology, the Second Affiliated Hospital of Anhui Medical University, Hefei 230601, China
Correspondence to: Wei Wei:,
DOI: 10.1038/s41401-018-0049-z
Received: 28 December 2017
Accepted: 20 May 2018
Advance online: 19 June 2018


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.
Keywords: G protein-coupled receptors; G protein coupling receptor kinases; Breast cancer; Prostate cancer; Hepatocellular carcinoma; Lung cancer

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