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Teaching old receptors new tricks: biasing seven-transmembrane receptors
Open accessAbstract
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, β-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 β-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 β-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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Metadata
- Authors
- Rajagopal, S., Rajagopal, K., & Lefkowitz, R. J.
- Venue
- Nature Reviews Drug Discovery
- Published
- 2010-05
- Volume
- 9
- Issue
- 5
- Pages
- 373-386
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2147196684
- Cited by
- 825
- References
- 0
- FWCI
- 5.30
- Type
- journal article
- Language
- en
- Open access
- green
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