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A cellular perspective of bias at G protein-coupled receptors.
Protein Science ( IF 4.5 ) Pub Date : 2020-04-16 , DOI: 10.1002/pro.3872
Thomas J Fernandez 1 , Monica De Maria 1 , Braden T Lobingier 1
Affiliation  

G protein-coupled receptors (GPCRs) modulate cell function over short- and long-term timescales. GPCR signaling depends on biochemical parameters that define the what, when, and where of receptor function: what proteins mediate and regulate receptor signaling, where within the cell these interactions occur, and how long these interactions persist. These parameters can vary significantly depending on the activating ligand. Collectivity, differential agonist activity at a GPCR is called bias or functional selectivity. Here we review agonist bias at GPCRs with a focus on ligands that show dramatically different cellular responses from their unbiased counterparts.

中文翻译:

细胞对G蛋白偶联受体的偏见。

G蛋白偶联受体(GPCR)在短期和长期时间内调节细胞功能。GPCR信号取决于生化参数,这些参数定义了受体功能的组成,时间和位置:什么蛋白质介导和调节受体信号传导,这些相互作用在细胞中的何处发生以及这些相互作用持续了多长时间。这些参数可以根据活化配体而显着变化。GPCR的集体性,差异性激动剂活性称为偏倚或功能选择性。在这里,我们回顾了在GPCR上的激动剂偏向,重点是显示出与无偏见的配体相比细胞反应截然不同的配体。
更新日期:2020-04-16
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