Seven-transmembrane receptors: crystals clarify

Trends Pharmacol Sci. 2002 Mar;23(3):140-6. doi: 10.1016/S0165-6147(00)01973-8.


The X-ray structure of the photoreceptor rhodopsin has provided the first atomic-resolution structure of a seven-transmembrane (7-TM) G-protein-coupled receptor. This has provided an improved template for interpreting the huge body of structure--activity, mutagenesis and affinity labelling data available for related 7-TM receptors, such as muscarinic acetylcholine receptors. Ligand contacts, and the intramolecular interactions that stabilize the ground state structure, can be identified with some degree of confidence. We now have a firm basis for attempts to predict the structure of the receptor--G-protein complex, and understand the mechanism by which the agonist--receptor complex activates the G protein.

Publication types

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

MeSH terms

  • Binding Sites
  • Crystallography, X-Ray
  • GTP-Binding Proteins
  • Humans
  • Ligands
  • Mutagenesis, Site-Directed
  • Protein Binding
  • Protein Conformation*
  • Receptors, Cell Surface / chemistry*
  • Receptors, Cell Surface / genetics
  • Receptors, G-Protein-Coupled*
  • Rhodopsin / chemistry
  • Rhodopsin / genetics


  • Ligands
  • Receptors, Cell Surface
  • Receptors, G-Protein-Coupled
  • seven-transmembrane G-protein-coupled receptor
  • Rhodopsin
  • GTP-Binding Proteins