The Metabolic Role of GRK2 in Insulin Resistance and Associated Conditions

Cells. 2021 Jan 15;10(1):167. doi: 10.3390/cells10010167.

Abstract

Insulin resistance (IRES) is a pathophysiological condition characterized by the reduced response to insulin of several tissues, including myocardial and skeletal muscle. IRES is associated with obesity, glucose intolerance, dyslipidemia, and hypertension, evolves toward type 2 diabetes, and increases the risk of developing cardiovascular diseases. Several studies designed to explore the mechanisms involved in IRES allowed the identification of a multitude of potential molecular targets. Among the most promising, G Protein Coupled Receptor Kinase type 2 (GRK2) appears to be a suitable one given its functional implications in many cellular processes. In this review, we will discuss the metabolic role of GRK2 in those conditions that are characterized by insulin resistance (diabetes, hypertension, heart failure), and the potentiality of its inhibition as a therapeutic strategy to revert both insulin resistance and its associated phenotypes.

Keywords: GRK2; diabetes; heart failure; hypertension; insulin resistance.

Publication types

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

MeSH terms

  • Animals
  • Diabetes Mellitus / metabolism*
  • Diabetes Mellitus, Type 2 / metabolism
  • G-Protein-Coupled Receptor Kinase 2 / metabolism*
  • Heart Failure / metabolism*
  • Humans
  • Hypertension / metabolism*
  • Inflammation
  • Insulin / metabolism
  • Insulin Resistance*
  • Insulin-Secreting Cells
  • Mice
  • Muscle, Skeletal / metabolism
  • Myocardium / metabolism
  • Peptides / chemistry
  • Phenotype
  • Phosphorylation
  • Risk
  • Signal Transduction

Substances

  • Insulin
  • Peptides
  • GRK2 protein, human
  • GRK2 protein, mouse
  • G-Protein-Coupled Receptor Kinase 2