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

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Abdul-Ridha, Alaa and Lane, J. Robert and Mistry, Shailesh N. and Lopez, Laura and Sexton, Patrick M. and Scammells, Peter J. and 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
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: https://doi.org/10.1074/jbc.M114.604967
Depositing User: Mistry, Dr Shailesh
Date Deposited: 09 Oct 2015 12:14
Last Modified: 26 Jun 2018 12:30
URI: http://eprints.nottingham.ac.uk/id/eprint/30312

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