A tale of detergent tails: GPCR activation beyond ligands

Structure. 2025 Apr 3;33(4):633-635. doi: 10.1016/j.str.2025.03.005.

Abstract

In this issue of Structure, Banerjee et al.1 use single-molecule FRET to explore how various detergents and cholesterol influence the conformational dynamics of the extracellular domain of the metabotropic glutamate receptor 2 (mGluR2). They show that the local membrane environment modulates the receptor's active-inactive state equilibrium and identifies specific cholesterol-binding sites, offering insights into potential drug-targeting strategies for mGluR2.

Publication types

  • Comment

MeSH terms

  • Binding Sites
  • Cholesterol / chemistry
  • Cholesterol / metabolism
  • Detergents* / chemistry
  • Detergents* / pharmacology
  • Fluorescence Resonance Energy Transfer
  • Humans
  • Ligands
  • Protein Binding
  • Receptors, Metabotropic Glutamate* / chemistry
  • Receptors, Metabotropic Glutamate* / metabolism

Substances

  • Receptors, Metabotropic Glutamate
  • Detergents
  • metabotropic glutamate receptor 2
  • Ligands
  • Cholesterol