GPCRs: Emerging anti-cancer drug targets

Cell Signal. 2018 Jan;41:65-74. doi: 10.1016/j.cellsig.2017.09.005. Epub 2017 Sep 18.


G protein-coupled receptors (GPCRs) constitute the largest and most diverse protein family in the human genome with over 800 members identified to date. They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis. Consequently, aberrant receptor activity has been demonstrated in numerous disorders/diseases, and as a result GPCRs have become the most successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic disorders. Many independent studies have also demonstrated a key role for GPCRs in tumourigenesis, establishing their involvement in cancer initiation, progression, and metastasis. Given the growing appreciation of the role(s) that GPCRs play in cancer pathogenesis, it is surprising to note that very few GPCRs have been effectively exploited in pursuit of anti-cancer therapies. The present review provides a broad overview of the roles that various GPCRs play in cancer growth and development, highlighting the potential of pharmacologically modulating these receptors for the development of novel anti-cancer therapeutics.

Keywords: Cancer; Drug discovery; Drug targets; GPCR; Signalling.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Disease Progression
  • Drug Discovery
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Mice
  • Molecular Targeted Therapy*
  • Neoplasms / drug therapy*
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*


  • Antineoplastic Agents
  • Receptors, G-Protein-Coupled