Current status of G-protein coupled receptors as potential targets against type 2 diabetes mellitus

Int J Biol Macromol. 2018 Oct 15;118(Pt B):2237-2244. doi: 10.1016/j.ijbiomac.2018.07.091. Epub 2018 Jul 17.

Abstract

GPCRs are among the most abundant surface receptors that play diverse roles including cell signalling and molecular transportation. They are major therapeutic receptor targets against various diseases like cancer and diabetes. A number of new GPCRs are being consistently being identified and deorphanised. Among them, some GPCRs are constitutively expressed while others are down-regulated. New therapeutic agents in the form of small molecule, synthetic peptides, and recombinant nucleic acids and proteins act as antagonists and agonists against various GPCR targets that potentially regulate glucose homeostasis. In the current review, we intend to summarize the various categories of GPCRs. At the same time, we intend to highlight the major GPCRs that have been targeted by various pharmaceutical companies against diabetes mellitus. In addition, we intended to summarize the most recently identified orphan GPCRs and their therapeutic potential against diabetes.

Keywords: Diabetes mellitus; GPCR; Therapeutic targets.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Humans
  • Hypoglycemic Agents / therapeutic use
  • Molecular Targeted Therapy*
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / metabolism*

Substances

  • Hypoglycemic Agents
  • Receptors, G-Protein-Coupled