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The Role of G Protein-coupled Receptor Kinases in Cancer

Shan Yu1, Litao Sun2, Yufei Jiao3

  • 1Centre of Reproduction Development and Aging, Faculty of Health Sciences, University of Macau, Taipa, Macau.

International Journal of Biological Sciences
|February 28, 2018
PubMed

Insights

G protein-coupled receptor kinases (GRKs) regulate cancer progression by modulating G protein-coupled receptor (GPCR) signaling and other pathways. Targeting GRKs offers a promising new therapeutic strategy for various cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial plasma membrane receptors involved in cancer biology.
  • GPCR signaling influences cancer aspects like vascular remodeling, invasion, and migration.
  • GPCR-targeted drugs represent a potential therapeutic strategy for diverse cancers.

Purpose of the Study:

  • To review the role of G protein-coupled receptor kinases (GRKs) in cell signaling.
  • To elucidate the involvement of GRKs in cancer progression.
  • To discuss the therapeutic potential of targeting GRKs in cancer treatment.

Main Methods:

  • Literature review of studies on GPCRs and GRKs in cancer.
  • Analysis of GRK mechanisms in modulating GPCR and non-GPCR signaling pathways.
  • Evaluation of therapeutic strategies targeting GRKs.

Main Results:

  • GRKs modulate GPCR signaling via phosphorylation, leading to desensitization and internalization.
  • This process inhibits downstream signaling pathways critical for cancer progression.
  • GRKs also regulate non-GPCR substrates, impacting other pathophysiological pathways relevant to cancer.

Conclusions:

  • GRKs play a significant role in regulating cell signaling and cancer progression.
  • Targeting GRKs presents a viable therapeutic approach for developing novel anti-cancer drugs.
Keywords:
CancerCell signalingG protein-coupled receptor (GPCR)G protein-coupled receptor kinase (GRK)

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