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Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor

Spurny, Radovan, Debaveye, Sarah, Farinha, Ana, Veys, Ken, Vos, Ann M., Gossas, Thomas, Atack, John, Bertrand, Sonia, Bertrand, Daniel, Danielson, U. Helena, Tresadern, Gary and Ulens, Chris 2015. Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America 112 (19) , E2543. 10.1073/pnas.1418289112

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Abstract

In this study we take advantage of a recently described chimera of the α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding protein (AChBP), termed α7-AChBP. To date, more than 70 crystal structures have been determined for AChBP in complex with ligands that occupy the orthosteric binding site. Here, we use an innovative screening strategy to discover molecular fragments that occupy allosteric binding sites. In combination with X-ray crystallography we determine a molecular blueprint of three different allosteric sites in α7-AChBP. Using electrophysiological recordings on the human α7 nAChR we demonstrate that each of the three sites is involved in allosteric modulation of the receptor. Our study contributes to understanding the sites of allosteric binding in ion channels.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Publisher: National Academy of Sciences
ISSN: 0027-8424
Date of Acceptance: 13 March 2015
Last Modified: 12 Mar 2019 13:50
URI: http://orca.cf.ac.uk/id/eprint/105858

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