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Int J Biol Sci 2018; 14(2):189-203. doi:10.7150/ijbs.22896


The Role of G Protein-coupled Receptor Kinases in Cancer

Shan Yu1, Litao Sun2, Yufei Jiao3, Leo Tsz On Lee1✉

1. Centre of Reproduction Development and Aging, Faculty of Health Sciences, University of Macau, Taipa, Macau
2. Department of Ultrasound, The Secondary Affiliated Hospital of Harbin Medical University, Harbin, China
3. Department of Pathology, The Secondary Affiliated Hospital of Harbin Medical University, Harbin, China


G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors. Emerging evidence demonstrates that signaling through GPCRs affects numerous aspects of cancer biology such as vascular remolding, invasion, and migration. Therefore, development of GPCR-targeted drugs could provide a new therapeutic strategy to treating a variety of cancers. G protein-coupled receptor kinases (GRKs) modulate GPCR signaling by interacting with the ligand-activated GPCR and phosphorylating its intracellular domain. This phosphorylation initiates receptor desensitization and internalization, which inhibits downstream signaling pathways related to cancer progression. GRKs can also regulate non-GPCR substrates, resulting in the modulation of a different set of pathophysiological pathways. In this review, we will discuss the role of GRKs in modulating cell signaling and cancer progression, as well as the therapeutic potential of targeting GRKs.

Keywords: G protein-coupled receptor (GPCR), G protein-coupled receptor kinase (GRK), Cancer, Cell signaling

This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license ( See for full terms and conditions.
How to cite this article:
Yu S, Sun L, Jiao Y, Lee LTO. The Role of G Protein-coupled Receptor Kinases in Cancer. Int J Biol Sci 2018; 14(2):189-203. doi:10.7150/ijbs.22896. Available from