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.
Highlights
Insulin is a peptide hormone produced in the pancreas by the β cells of the Langerhans islets in response to the increase in plasma glucose levels
G Protein Coupled Receptor Kinase type 2 (GRK2) mediates adrenergic insulin resistance while its inhibition increases insulin sensitivity [35]. These observations point to GRK2 as a potential target, considering that conditions associated with insulin resistance, are all characterized by elevated kinase levels
A growing number of molecular mechanisms could hypothetically be targeted through pharmacological approaches for the treatments of insulin resistance and associated pathologies
Summary
Insulin is a peptide hormone produced in the pancreas by the β cells of the Langerhans islets in response to the increase in plasma glucose levels. It induces the rapid absorption of glucose, protein, and fatty acids by tissues for metabolism, storage, and energy production [1] (Figure 1). Alterations in insulin signaling and production, as observed in insulin resistance, significantly impair glucose homeostasis in several pathological conditions, such as diabetes, hypertension, and heart failure. G Protein Coupled Receptor Kinase type 2 (GRK2) has been identified as a mechanism of impaired glucose homeostasis in insulin resistance and its complications. We will discuss the metabolic role of GRK2 in insulin resistance related conditions.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
