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Biased signaling as allosteric probe dependence
Cellular Signalling ( IF 4.4 ) Pub Date : 2020-11-24 , DOI: 10.1016/j.cellsig.2020.109844
Terry Kenakin 1
Affiliation  

Signaling ‘bias’ is a phenomenon whereby the natural allosteric probe dependence of seven transmembrane receptors allows different receptor conformations (stabilized by different agonists) to activate some signaling pathways (coupled to pleiotropically coupled receptors) more than others at the expense of those other pathways. There are a number of relevant scenarios where such an activity could be therapeutically beneficial therefore there are practical reasons why this property of receptors should be exploited. This paper discusses recent ideas around attempts to harness this potentially useful idea and also the limitations around the current methods available to do so. Specifically, the determination of a quantitative value for the receptor bias of a given agonist that may translate to useful in vivo has been particularly elusive and studies need to be directed to solving this problem.



中文翻译:

偏向信号作为变构探针依赖性

信号传导“偏差”是一种现象,其中七种跨膜受体的天然变构探针依赖性允许不同的受体构象(由不同的激动剂稳定)比其他途径更多地激活某些信号传导途径(与多效性耦合受体耦合),而牺牲其他途径。在许多相关情况下,这种活性可能对治疗有益,因此有实际原因说明应该利用受体的这种特性。本文讨论了围绕尝试利用这一潜在有用想法的最新想法,以及当前可用方法的局限性。具体来说,

更新日期:2020-12-22
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