Lu_2002_Trends.Pharmacol.Sci_23_140

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.