Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
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- erati...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Published: |
American Society for Biochemistry and Molecular Biology
2014
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| Online Access: | https://eprints.nottingham.ac.uk/30415/ |
| _version_ | 1848793980908601344 |
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| author | Abdul-Ridha, Alaa López, Laura Keov, Peter Thal, David M. Mistry, Shailesh N. Sexton, Patrick M. Lane, J. Robert Canals, Meritxell Christopoulos, Arthur |
| author_facet | Abdul-Ridha, Alaa López, Laura Keov, Peter Thal, David M. Mistry, Shailesh N. Sexton, Patrick M. Lane, J. Robert Canals, Meritxell Christopoulos, Arthur |
| author_sort | Abdul-Ridha, Alaa |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T19:08:55Z |
| format | Article |
| id | nottingham-30415 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:08:55Z |
| publishDate | 2014 |
| publisher | American Society for Biochemistry and Molecular Biology |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-304152020-05-04T16:41:33Z https://eprints.nottingham.ac.uk/30415/ Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor Abdul-Ridha, Alaa López, Laura Keov, Peter Thal, David M. Mistry, Shailesh N. Sexton, Patrick M. Lane, J. Robert Canals, Meritxell Christopoulos, Arthur 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. American Society for Biochemistry and Molecular Biology 2014-01-17 Article PeerReviewed Abdul-Ridha, Alaa, López, Laura, Keov, Peter, Thal, David M., Mistry, Shailesh N., Sexton, Patrick M., Lane, J. Robert, 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 http://www.jbc.org/content/289/9/6067 doi:10.1074/jbc.M113.539080 doi:10.1074/jbc.M113.539080 |
| spellingShingle | Abdul-Ridha, Alaa López, Laura Keov, Peter Thal, David M. Mistry, Shailesh N. Sexton, Patrick M. Lane, J. Robert Canals, Meritxell Christopoulos, Arthur Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title | Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title_full | Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title_fullStr | Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title_full_unstemmed | Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title_short | Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor |
| title_sort | molecular determinants of allosteric modulation at the m1 muscarinic acetylcholine receptor |
| url | https://eprints.nottingham.ac.uk/30415/ https://eprints.nottingham.ac.uk/30415/ https://eprints.nottingham.ac.uk/30415/ |