Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
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 mode...
| Main Authors: | , , , , , , , |
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| Format: | Article |
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American Society for Biochemistry and Molecular Biology
2014
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| Online Access: | https://eprints.nottingham.ac.uk/30312/ |
| _version_ | 1848793961415573504 |
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| author | Abdul-Ridha, Alaa Lane, J. Robert Mistry, Shailesh N. Lopez, Laura Sexton, Patrick M. Scammells, Peter J. Christopoulos, Arthur Canals, Meritxell |
| author_facet | Abdul-Ridha, Alaa Lane, J. Robert Mistry, Shailesh N. Lopez, Laura Sexton, Patrick M. Scammells, Peter J. Christopoulos, Arthur Canals, Meritxell |
| author_sort | Abdul-Ridha, Alaa |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T19:08:37Z |
| format | Article |
| id | nottingham-30312 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:08:37Z |
| publishDate | 2014 |
| publisher | American Society for Biochemistry and Molecular Biology |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-303122020-05-04T16:55:34Z https://eprints.nottingham.ac.uk/30312/ Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor Abdul-Ridha, Alaa Lane, J. Robert Mistry, Shailesh N. Lopez, Laura Sexton, Patrick M. Scammells, Peter J. Christopoulos, Arthur Canals, Meritxell 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. American Society for Biochemistry and Molecular Biology 2014-10-17 Article PeerReviewed 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 http://www.jbc.org/content/289/48/33701 doi:10.1074/jbc.M114.604967 doi:10.1074/jbc.M114.604967 |
| spellingShingle | Abdul-Ridha, Alaa Lane, J. Robert Mistry, Shailesh N. Lopez, Laura Sexton, Patrick M. Scammells, Peter J. Christopoulos, Arthur Canals, Meritxell Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title | Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title_full | Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title_fullStr | Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title_full_unstemmed | Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title_short | Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor |
| title_sort | mechanistic insights into allosteric structure-function relationships at the m1 muscarinic acetylcholine receptor |
| url | https://eprints.nottingham.ac.uk/30312/ https://eprints.nottingham.ac.uk/30312/ https://eprints.nottingham.ac.uk/30312/ |