Article
Structure of a beta1-adrenergic G-protein-coupled receptor.
Nature - 24 Jul 2008
Warne Tony, Serrano-Vega Maria J, Baker Jillian G, Moukhametzianov Rouslan, Edwards Patricia C, Henderson Richard, Leslie Andrew G W, Tate Christopher G, Schertler Gebhard F X
Abstract excerpt
G-protein-coupled receptors have a major role in transmembrane signalling in most eukaryotes and many are important drug targets. Here we report the 2.7 A resolution crystal structure of a beta(1)-adrenergic receptor in complex with the high-affinity antagonist cyanopindolol. The modified turkey (Meleagris gallopavo) receptor was selected to be in its antagonist conformation and its thermostability improved by...
Topics
- Adrenergic beta-1 Receptor Agonists
- Adrenergic beta-1 Receptor Antagonists
- Adrenergic beta-Antagonists
- Amino Acid Motifs
- Animals
- Binding Sites
- Crystallization
- Crystallography, X-Ray
- Ligands
- Models, Molecular