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Advances in G Protein-Coupled Receptor Allostery: From Function to Structure by Arthur Christopoulos is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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It is now widely accepted that G protein-coupled receptors (GPCRs) are highly dynamic proteins that adopt multiple active states linked to distinct functional outcomes. Furthermore, these states can be differentially stabilized not only by orthosteric ligands but also by allosteric ligands acting at spatially distinct binding sites. The key pharmacologic characteristics of GPCR allostery include improved selectivity due to either greater sequence divergence between receptor subtypes and/or subtype-selective cooperativity, a ceiling level to the effect, probe dependence (whereby the magnitude and direction of the allosteric effect change with the nature of the interacting ligands), and the potential for biased signaling.Recent chemical biology developments are beginning to demonstrate how the incorporation of analytical pharmacology and operational modeling into the experimental workflow can enrich structure-activity studies of allostery and bias, and have also led to the discovery of a new class of hybrid orthosteric/ allosteric (bitopic) molecules. The potential for endogenous allosteric modulators to play a role in physiology and disease remains to be fully appreciated but will l

Who reads Advances in G Protein-Coupled Receptor Allostery: From Function to Structure?

Author

Arthur Christopoulos

Publisher

American Society for Pharmacology & Experimental Therapeutics (ASPET)

Published

2014

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)