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Christopher, JA, Aves, SJ, Bennett, KA, Doré, AS, Errey, JC, Jazayeri, A, Marshall, FH, Okrasa, K, Serrano-Vega, MJ, Tehan, B, Wiggin, GR & Congreve, M.

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The adenosine A2A receptor (shown here as a bundle of helical ribbons) is presented on the surface of many neuronal cells. Molecules known to bind to the A2A receptor include xanthines, such as caffeine (shown here as ball and stick models), and modified xanthines have been developed as potential treatments for neurodegenerative disorders such as Parkinson’s disease. Generation of an adenosine A2A StaR® led to the determination of its structure with caffeine bound, allowing visualisation of the interactions between caffeine and its receptor, and enabling potential new therapeutic molecules to be discovered.

Structure, Volume 19, Issue 9, Doré A.S. et al. Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine. Pp 1283-1293. Copyright Elsevier Ltd. All rights reserved. (2011)

Electron density around the cyanopindolol ligand binding site in the beta 1 adrenergic receptor.

Acknowledgements. Warne et al, Nature. 2008.

Target GPCR crystals grown by the lipidic cubic phase method at Heptares Therapeutics.

Acknowledgements. Andrew Doré, Heptares Therapeutics Ltd, UK.

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