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Nat Rev Drug Discov. 2010 May;9(5):373-86. doi: 10.1038/nrd3024.

Teaching old receptors new tricks: biasing seven-transmembrane receptors.

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  • 1Department of Medicine, Duke University Medical Center, 2301 Erwin Road, Durham, North Carolina 27710, USA.


Seven-transmembrane receptors (7TMRs; also known as G protein-coupled receptors) are the largest class of receptors in the human genome and are common targets for therapeutics. Originally identified as mediators of 7TMR desensitization, beta-arrestins (arrestin 2 and arrestin 3) are now recognized as true adaptor proteins that transduce signals to multiple effector pathways. Signalling that is mediated by beta-arrestins has distinct biochemical and functional consequences from those mediated by G proteins, and several biased ligands and receptors have been identified that preferentially signal through either G protein- or beta-arrestin-mediated pathways. These ligands are not only useful tools for investigating the biochemistry of 7TMR signalling, they also have the potential to be developed into new classes of therapeutics.

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