Teaching old receptors new tricks: biasing seven-transmembrane receptors.
Teaching old receptors new tricks: biasing seven-transmembrane receptors.
复制标题
DOI：
10.1038/nrd3024
复制
发表时间：
2010-05
期刊：
影响因子：
--
通讯作者：
中科院分区：
文献类型：
--
作者：
七跨膜受体(7TMR；也称为G蛋白偶联受体)是人类基因组中最大的一类受体，也是治疗的常见靶点。β-arrestins(arrestin 2和arrestin 3)最初被认为是7TMR脱敏的介体，现在被认为是真正的接头蛋白，可以将信号传递到多个效应通路。由β-arrestins介导的信号转导与由G蛋白介导的信号转导具有不同的生化和功能后果，已发现几种有偏见的配体和受体优先通过G蛋白或β-arrestin介导的途径转导信号。这些配体不仅是研究7TMR信号生物化学的有用工具，而且它们还有可能被开发成新的治疗类别。
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.