Seven-transmembrane receptors: crystals clarify.
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.
Lu
Zhi-Liang
ZL
MRC Human Reproductive Sciences Unit, Centre for Reproductive Biology, Edinburgh, UK.
Saldanha
Jose W
JW
Hulme
Edward C
EC
D001665:Binding Sites; D018360:Crystallography, X-Ray; D019204:GTP-Binding Proteins; D006801:Humans; D008024:Ligands; D016297:Mutagenesis, Site-Directed; D011485:Protein Binding; D011487:Protein Conformation; D011956:Receptors, Cell Surface / Q000737:chemistry* / Q000235:genetics; D043562:Receptors, G-Protein-Coupled; D012243:Rhodopsin / Q000737:chemistry / Q000235:genetics
D008024:Ligands; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C450520:seven-transmembrane G-protein-coupled receptor; D012243:Rhodopsin; D019204:GTP-Binding Proteins