[HTML][HTML] A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation
The Monod-Wyman-Changeux (MWC) model was initially proposed to describe the
allosteric properties of regulatory enzymes and subsequently extended to receptors. Yet
despite GPCRs representing the largest family of receptors and drug targets, no study has
systematically evaluated the MWC mechanism as it applies to GPCR allosteric ligands. We
reveal how the recently described allosteric modulator, benzyl quinolone carboxylic acid
(BQCA), behaves according to a strict, two-state MWC mechanism at the M 1 muscarinic …
allosteric properties of regulatory enzymes and subsequently extended to receptors. Yet
despite GPCRs representing the largest family of receptors and drug targets, no study has
systematically evaluated the MWC mechanism as it applies to GPCR allosteric ligands. We
reveal how the recently described allosteric modulator, benzyl quinolone carboxylic acid
(BQCA), behaves according to a strict, two-state MWC mechanism at the M 1 muscarinic …