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Abdul-Ridha, Alaa; López, Laura; Keov, Peter; Thal, David M.; Mistry, Shailesh N.; Sexton, Patrick M.; Lane, J. Robert; Canals, Meritxell; Christopoulos, Arthur (2014)
Publisher: American Society for Biochemistry and Molecular Biology
Languages: English
Types: Article
Subjects: Signal Transduction
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.

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