Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor
Article, Other literature type
Thal, David M.
Mistry, Shailesh N.
Sexton, Patrick M.
Lane, J. Robert
- Publisher: American Society for Biochemistry and Molecular Biology
Background: BQCA is a selective allosteric modulator of the M1 mAChR.\ud Results: Residues that govern BQCA activity were identified using mutagenesis and molecular modelling.\ud Conclusion: BQCA likely occupies a pocket overlapping prototypical mAChR modulators and gains selectivity through coop- erativity with orthosteric ligands.\ud Significance: Understanding the structural basis of BQCA function can provide insight into the design of more tailored allosteric ligands.