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Instruments / Technical Area	Publication Details	Published	Actions
I24-Microfocus Macromolecular Crystallography	Structure of the adenosine A2A receptor in complex with ZM241385 and the xanthines XAC and caffeine Andrew S. Dore , Nathan Robertson , James C. Errey , Irene Ng , Kaspar Hollenstein , Ben Tehan , Edward Hurrell , Kirstie Bennett , Miles Congreve , Francesca Magnani , Christopher G. Tate , Malcolm Weir , Fiona H. Marshall Structure 19 (9), 1283 - 1293 DOI: 10.1016/j.str.2011.06.014 PMID: 21885291 Diamond Proposal Number(s): [6641] Show Abstract ▼ Abstract: Methylxanthines, including caffeine and theophylline, are among the most widely consumed stimulant drugs in the world. These effects are mediated primarily via blockade of adenosine receptors. Xanthine analogs with improved properties have been developed as potential treatments for diseases such as Parkinson's disease. Here we report the structures of a thermostabilized adenosine A2A receptor in complex with the xanthines xanthine amine congener and caffeine, as well as the A2A selective inverse agonist ZM241385. The receptor is crystallized in the inactive state conformation as defined by the presence of a salt bridge known as the ionic lock. The complete third intracellular loop, responsible for G protein coupling, is visible consisting of extended helices 5 and 6. The structures provide new insight into the features that define the ligand binding pocket of the adenosine receptor for ligands of diverse chemotypes as well as the cytoplasmic regions that interact with signal transduction proteins.	Sep 2011

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I24-Microfocus Macromolecular Crystallography

Structure of the adenosine A2A receptor in complex with ZM241385 and the xanthines XAC and caffeine