Seven-transmembrane receptors: crystals clarify

被引:140
作者
Lu, ZL
Saldanha, JW
Hulme, EC
机构
[1] MRC, Ctr Reprod Biol, Reprod Biol Unit, Edinburgh, Midlothian, Scotland
[2] Natl Inst Med Res, Div Phys Biochem, London NW7 1AA, England
基金
英国医学研究理事会;
关键词
D O I
10.1016/S0165-6147(00)01973-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
dThe X-ray structure of the photo receptor 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.
引用
收藏
页码:140 / 146
页数:7
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