RGD Reference Report - Teaching old receptors new tricks: biasing seven-transmembrane receptors. - Rat Genome Database

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

Authors: Rajagopal, S  Rajagopal, K  Lefkowitz, RJ 
Citation: Rajagopal S, etal., Nat Rev Drug Discov. 2010 May;9(5):373-86.
RGD ID: 5130117
Pubmed: PMID:20431569   (View Abstract at PubMed)
PMCID: PMC2902265   (View Article at PubMed Central)
DOI: DOI:10.1038/nrd3024   (Journal Full-text)

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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