CHAPTER 5: Examining Allosterism in a Dimeric G-Protein-Coupled Receptor Context

Jesús Giraldo, Jordi Ortiz, James Dalton, Bin Zhou

Research output: Chapter in BookChapterResearchpeer-review


© The Royal Society of Chemistry 2017. 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.
Original languageEnglish
Title of host publicationRSC Drug Discovery Series
Number of pages33
ISBN (Electronic)2041-3211
Publication statusPublished - 1 Jan 2017


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