title: Teaching old receptors new tricks: biasing seven-transmembrane receptors.
abstract: 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.
authors.affiliation: Department of Medicine, Duke University Medical Center, 2301 Erwin Road, Durham, North Carolina 27710, USA.
authors.forename: Sudarshan
authors.initials: S
authors.lastname: Rajagopal
authors.forename: Keshava
authors.initials: K
authors.lastname: Rajagopal
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Lefkowitz
mesh_terms: D000818:Animals; D019390:Arrestins / Q000378:metabolism*; D016503:Drug Delivery Systems; D015195:Drug Design; D015894:Genome, Human; D006801:Humans; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects; D000071557:beta-Arrestins
chemical_list: D019390:Arrestins; D008024:Ligands; D043562:Receptors, G-Protein-Coupled; C082333:arrestin3; D000071557:beta-Arrestins; C450520:seven-transmembrane G-protein-coupled receptor