The third intracellular loop of GPCRs: size matters

  • Trends Pharmacol Sci. 2023 Aug;44(8):492-494. doi: 10.1016/j.tips.2023.05.001.
Jürgen Wess  1
Affiliations
  • 1. Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bldg. 8A, 8 Center Drive MSC 0810, Bethesda, MD 20892, USA. Electronic address: [email protected].
PMID: 37208206 DOI: 10.1016/j.tips.2023.05.001
Abstract

The third intracellular loop of G-protein-coupled receptors (GPCRs) shows remarkable diversity in sequence and overall length. Sadler and colleagues recently demonstrated that this domain acts as an 'autoregulator' of receptor activity and that its length contributes to receptor/G-protein coupling selectivity. These observations may prove useful for developing novel therapeutics.

Keywords
G-protein; receptor conformation; receptor structure; signal transduction.