Seven-transmembrane receptors: crystals clarify
Zhi-Liang Lu1, Jose W Saldanha, Edward C Hulme
1MRC Human Reproductive Sciences Unit, Centre for Reproductive Biology, Edinburgh, UK.
Abstract:
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.
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