Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor

Abdul-Ridha, Alaa and López, Laura and Keov, Peter and Thal, David M. and Mistry, Shailesh N. and Sexton, Patrick M. and Lane, J. Robert and Canals, Meritxell and Christopoulos, Arthur (2014) Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry, 289 (9). pp. 6067-6079. ISSN 0021-9258

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Abstract

Background: BQCA is a selective allosteric modulator of the M1 mAChR.

Results: Residues that govern BQCA activity were identified using mutagenesis and molecular modelling.

Conclusion: BQCA likely occupies a pocket overlapping prototypical mAChR modulators and gains selectivity through coop- erativity with orthosteric ligands.

Significance: Understanding the structural basis of BQCA function can provide insight into the design of more tailored allosteric ligands.

Item Type: Article
Additional Information: This research was originally published in Journal of Biological Chemistry. Alaa Abdul-Ridha, Laura López, Peter Keov, David M. Thal, Shailesh N. Mistry, Patrick M. Sexton, Meritxell Canals and Arthur Christopoulos. Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry. 2014. 289:6067-6079. © the American Society for Biochemistry and Molecular Biology.
Schools/Departments: University of Nottingham UK Campus > Faculty of Science > School of Pharmacy
Identification Number: https://doi.org/10.1074/jbc.M113.539080
Depositing User: Mistry, Dr Shailesh
Date Deposited: 09 Oct 2015 12:12
Last Modified: 14 Sep 2016 14:42
URI: http://eprints.nottingham.ac.uk/id/eprint/30415

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