Full Text | PDF

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

Review

The Role of G Protein-coupled Receptor Kinases in Cancer

Shan Yu¹, Litao Sun², Yufei Jiao³, Leo Tsz On Lee^1✉

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

✉ Corresponding author: Leo T.O. Lee, Centre of Reproduction, Development and Aging, Faculty of Health Sciences, University of Macau, Taipa, Macau, China; E-mail: LTOLeemo

Abstract

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

Citation styles

©2025 Ivyspring International Publisher. Terms of use