The Role of G Protein-coupled Receptor Kinases in the Pathology of Malignant Tumors

Overview

Journal Acta Pharmacol Sin

Specialty Pharmacology

Date 2018 Jun 21

PMID 29921886

Citations 11

Authors

Wu-Yi Sun

Jing-Jing Wu

Wen-Ting Peng

Jia-Chang Sun

Wei Wei

Affiliations

Soon will be listed here.

Abstract

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.

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