Emerging paradigms in GPCR allostery: implications for drug discovery

作者: Denise Wootten , Arthur Christopoulos , Patrick M. Sexton

DOI: 10.1038/NRD4052

关键词: Drug discoveryAllosteric regulationComputational biologyG protein-coupled receptorBiologyBioinformatics

摘要: Allosteric ligands bind to G protein-coupled receptors (GPCRs; also known as seven-transmembrane receptors) at sites that are distinct from the which endogenous bind. The existence of allosteric has enriched ways in functions GPCRs can be manipulated for potential therapeutic benefit, yet complexity their actions provides both challenges and opportunities drug screening development. Converging avenues research areas such biased signalling by mechanisms modulate effects diverse have provided new insights into how interactions between could exploited discovery. These findings alter drugs is performed may increase chances success development modulators clinical lead compounds.

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