Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor

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Abdul-Ridha, Alaa, Lane, J. Robert, Mistry, Shailesh N., Lopez, Laura, Sexton, Patrick M., Scammells, Peter J., Christopoulos, Arthur and Canals, Meritxell (2014) Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry, 289 (48). pp. 33701-33711. ISSN 0021-9258

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Abstract

Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described.

Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.

Conclusion: Combined analytical, structure-function, and modeling approaches uncover allosteric mechanisms at the M1 mAChR.

Significance: New chemical space can be explored in the development of tailored M1 mAChR PAMs.

Item Type: Article
RIS ID: https://nottingham-repository.worktribe.com/output/737982
Additional Information: This research was originally published in Journal of Biological Chemistry. Alaa Abdul-Ridha, J. Robert Lane, Shailesh N. Mistry, Laura López, Patrick M. Sexton, Peter J. Scammells, Arthur Christopoulos and Meritxell Canals. Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry. 2015. 289:33701-33711. © the American Society for Biochemistry and Molecular Biology.
Schools/Departments: University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number: 10.1074/jbc.M114.604967
Depositing User: Mistry, Dr Shailesh
Date Deposited: 09 Oct 2015 12:14
Last Modified: 04 May 2020 16:55
URI: https://eprints.nottingham.ac.uk/id/eprint/30312

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