Two neuroendocrine G protein-coupled receptor molecules, somatostatin and melatonin: Physiology of signal transduction and therapeutic perspectives

J Cell Physiol. 2021 Apr;236(4):2505-2518. doi: 10.1002/jcp.30062. Epub 2020 Sep 28.

Abstract

Recent studies have shown that G protein-coupled receptors (GPCRs), the largest signal-conveying receptor family, are targets for mutations occurring frequently in different cancer types. GPCR alterations associated with cancer development represent significant challenges for the discovery and the advancement of targeted therapeutics. Among the different molecules that can activate GPCRs, we focused on two molecules that exert their biological actions regulating many typical features of tumorigenesis such as cellular proliferation, survival, and invasion: somatostatin and melatonin. The modulation of signaling pathways, that involves these two molecules, opens an interesting scenario for cancer therapy, with the opportunity to act at different molecular levels. Therefore, the aim of this review is the analysis of the biological activity and the therapeutic potential of somatostatin and melatonin, displaying a high affinity for GPCRs, that interfere with cancer development and maintenance.

Keywords: GPCRs; melatonin; somatostatin; targeted therapies; tumors.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Ligands
  • Melatonin / metabolism*
  • Melatonin / therapeutic use
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*
  • Neoplasms / pathology
  • Receptors, Melatonin / metabolism*
  • Receptors, Somatostatin / metabolism*
  • Signal Transduction*
  • Somatostatin / metabolism*
  • Somatostatin / therapeutic use

Substances

  • Antineoplastic Agents
  • Ligands
  • Receptors, Melatonin
  • Receptors, Somatostatin
  • Somatostatin
  • Melatonin