Metabolic roles of G protein-coupled receptor signaling in obesity and type 2 diabetes

FEBS J. 2021 Apr;288(8):2622-2644. doi: 10.1111/febs.15800. Epub 2021 Mar 22.

Abstract

The incidence of obesity and type 2 diabetes (T2D) has been increasing steadily worldwide. It is estimated that by 2045 more than 800 million people will be suffering from diabetes. Despite the advancements in modern medicine, more effective therapies for treating obesity and T2D are needed. G protein-coupled receptors (GPCRs) have emerged as important drug targets for various chronic diseases, including obesity, T2D, and liver diseases. During the past two decades, many laboratories worldwide focused on understanding the role of GPCR signaling in regulating glucose metabolism and energy homeostasis. The information gained from these studies can guide the development of novel therapeutic agents. In this review, we summarize recent studies providing insights into the role of GPCR signaling in peripheral, metabolically important tissues such as pancreas, liver, skeletal muscle, and adipose tissue, focusing primarily on the use of mutant animal models and human data.

Keywords: G protein-coupled receptors; chronic diseases and glucose homeostasis; drug discovery; metabolism; nonalcoholic fatty liver disease; obesity; type 2 diabetes.

Publication types

  • Research Support, N.I.H., Intramural
  • Review

MeSH terms

  • Adipose Tissue / metabolism
  • Diabetes Mellitus, Type 2 / genetics*
  • Diabetes Mellitus, Type 2 / pathology
  • Homeostasis / genetics
  • Humans
  • Insulin Resistance / genetics*
  • Liver / metabolism
  • Obesity / genetics*
  • Obesity / pathology
  • Pancreas / metabolism
  • Receptors, G-Protein-Coupled / genetics*
  • Signal Transduction / genetics

Substances

  • Receptors, G-Protein-Coupled