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Examining Allosterism in a Dimeric G-Protein-Coupled Receptor Context

G-protein-coupled receptor (GPCR) allosterism is examined by comparing structure–function relationships in monomeric and dimeric receptor arrangements. The metabotropic glutamate receptors are chosen as a paradigm of dimeric receptors because there are no doubts about their dimeric nature both from structural and functional data. A number of mathematical models are revisited. The selected models offer a quantitative description of pharmacological properties, providing a mechanistic explanation of receptor subunits cross-talk and ligand cooperativity; thus, bringing in a conceptual framework for fitting experimental data and simulating mechanistic hypotheses. Further work is needed combining experimental (crystallography, nuclear magnetic resonance, fluorescence and bioluminescence) and theoretical (mathematics and computational-chemistry) efforts to fully understand the complex behaviour of GPCR allosteric machinery.

Print publication date: 24 Nov 2016
Copyright year: 2017
Print ISBN: 978-1-78262-459-2
PDF eISBN: 978-1-78262-927-6
ePub eISBN: 978-1-78262-969-6
From the book series:
Drug Discovery