期刊
NATURE REVIEWS DRUG DISCOVERY
卷 9, 期 5, 页码 373-386出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3024
关键词
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资金
- National Institutes of Health (NIH) [HL16037, HL70631, HL07101-34]
- NATIONAL HEART, LUNG, AND BLOOD INSTITUTE [R01HL016037, R01HL070631, R37HL016037, T32HL007101] Funding Source: NIH RePORTER
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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