TY - JOUR
T1 - Seven-transmembrane receptors
T2 - Crystals clarify
AU - Lu, Zhi Liang
AU - Saldanha, Jose W.
AU - Hulme, Edward C.
N1 - Funding Information:
We thank Rex Palmer of Birkbeck College, London, for assistance in the generation of the NMS coordinates. The figures shown in this manuscript were generated with the WebLab viewer. This work was supported by the Medical Research Council, UK.
PY - 2002/3/1
Y1 - 2002/3/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0036499727&partnerID=8YFLogxK
U2 - 10.1016/S0165-6147(00)01973-8
DO - 10.1016/S0165-6147(00)01973-8
M3 - Review article
C2 - 11879682
AN - SCOPUS:0036499727
SN - 0165-6147
VL - 23
SP - 140
EP - 146
JO - Trends in Pharmacological Sciences
JF - Trends in Pharmacological Sciences
IS - 3
ER -