A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation.

  title={A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation.},
  author={Meritxell Canals and J Robert Lane and Adriel Wen and Peter J. Scammells and Patrick M. Sexton and Arthur Christopoulos},
  journal={The Journal of biological chemistry},
  volume={287 1},
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… CONTINUE READING
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Conformational Selection and GPCR

  • C. W. Murray, D. C. Rees
  • Allostery JANUARY
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Conformational Selection and GPCR Allostery 658 JOURNAL OF BIOLOGICAL CHEMISTRY VOLUME

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