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lüll Teaching old receptors new tricks: biasing seven-transmembrane receptors Rajagopal S; Rajagopal K; Lefkowitz RJNat Rev Drug Discov 2010[May]; 9 (5): 373-86Seven-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.|*Drug Delivery Systems[MESH]|Animals[MESH]|Arrestins/*metabolism[MESH]|Drug Design[MESH]|Genome, Human[MESH]|Humans[MESH]|Ligands[MESH]|Receptors, G-Protein-Coupled/*metabolism[MESH]|Signal Transduction/drug effects[MESH]|beta-Arrestins[MESH] |