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Novel Allosteric Modulators of G Protein-coupled Receptors

Research output: Contribution to journalReviewResearchpeer-review

Patrick R Gentry, Patrick M Sexton, Arthur Christopoulos

G protein-coupled receptors (GPCRs) are allosteric proteins, because their signal transduction relies on interactions between topographically distinct, yet conformationally linked, domains. Much of the focus on GPCR allostery in the new millennium, however, has been on modes of targeting GPCR allosteric sites with chemical probes due to the potential for novel therapeutics. It is now apparent that some GPCRs possess more than one targetable allosteric site, in addition to a growing list of putative endogenous modulators. Advances in structural biology are also shedding new insights into mechanisms of allostery, although the complexities of candidate allosteric drugs necessitate rigorous biological characterization.

Original languageEnglish
JournalThe Journal of Biological Chemistry
Volume290
Issue number32
Pages (from-to)19478-88
Number of pages11
ISSN0021-9258
DOIs
Publication statusPublished - 7 Aug 2015
Externally publishedYes

Bibliographical note

© 2015 by The American Society for Biochemistry and Molecular Biology, Inc.

    Research areas

  • Allosteric Regulation, Allosteric Site/drug effects, Crystallography, X-Ray/history, Drug Design, History, 21st Century, Humans, Ligands, Models, Molecular, Protein Binding, Protein Structure, Tertiary, Receptors, G-Protein-Coupled/agonists, Signal Transduction, Small Molecule Libraries/chemical synthesis, Structure-Activity Relationship

ID: 213599236