Role and therapeutic potential of G-protein coupled receptors in breast cancer progression and metastases

Eur J Pharmacol. 2015 Sep 15;763(Pt B):178-83. doi: 10.1016/j.ejphar.2015.05.011. Epub 2015 May 14.


G-protein-coupled receptors (GPCRs) comprise a large family of cell-surface receptors, which have recently emerged as key players in tumorigenesis, angiogenesis and metastasis. In this review, we discussed our current understanding of the many roles played by GPCRs in general, and particularly Angiotensin II type I receptor (AGTR1), a member of the seven-transmembrane-spanning G-protein coupled receptor superfamily, and its significance in breast cancer progression and metastasis. We have also discussed different strategies for targeting AGTR1, and its ligand Angiotension II (Ang II), which might unravel unique opportunities for breast cancer prevention and treatment. For example, AGTR1 blockers (ARBs) which are already in clinical use for treating hypertension, merit further investigation as a therapeutic strategy for AGTR1-positive cancer patients and may have the potential to prevent Ang II-AGTR1 signalling mediated cancer pathogenesis and metastases.

Keywords: ACE; AGTR1; Breast cancer; GPCR; Metastases.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / genetics
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology*
  • Disease Progression*
  • Humans
  • Molecular Targeted Therapy
  • Neoplasm Metastasis
  • Receptors, G-Protein-Coupled / metabolism*


  • Receptors, G-Protein-Coupled