Where have all the active receptor states gone?

Nat Chem Biol. 2012 Jul 18;8(8):674-7. doi: 10.1038/nchembio.1024.

Abstract

Defining G protein-coupled receptor ligand efficacy and biased agonism in precise chemical terms is one challenge posed by the current structural data that exists for this receptor family. Concepts classically used for understanding enzymes and other nonreceptor proteins may lead us in the right direction.

MeSH terms

  • Allosteric Regulation
  • Animals
  • Arrestin / metabolism
  • Cell Membrane / chemistry
  • Cell Membrane / physiology
  • Drug Discovery
  • Gene Expression Regulation / physiology
  • Ligands
  • Models, Molecular
  • Protein Binding
  • Protein Conformation
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction

Substances

  • Arrestin
  • Ligands
  • Receptors, G-Protein-Coupled