Decay of an active GPCR: Conformational dynamics govern agonist rebinding and persistence of an active, yet empty, receptor state [Pharmacology],Proceedings of the National Academy of Sciences of the United States of America

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Decay of an active GPCR: Conformational dynamics govern agonist rebinding and persistence of an active, yet empty, receptor state [Pharmacology]
Proceedings of the National Academy of Sciences of the United States of America ( IF 9.4 ) Pub Date : 2016-10-18 09:32:52 , DOI: 10.1073/pnas.1606347113
Christopher T. Schafer ₁ , Jonathan F. Fay ₁ , Jay M. Janz ₁ , David L. Farrens ₁

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Here, we describe two insights into the role of receptor conformational dynamics during agonist release (all-trans retinal, ATR) from the visual G protein-coupled receptor (GPCR) rhodopsin. First, we show that, after light activation, ATR can continually release and rebind to any receptor remaining in an active-like conformation. As with other...

中文翻译：

主动GPCR的衰减：构象动力学控制激动剂的重新结合和主动但空的受体状态的持久性[药理学]

在这里，我们描述了从视觉G蛋白偶联受体（GPCR）视紫红质激动剂释放（全反式视网膜，ATR）期间受体构象动力学的作用的两种见解。首先，我们表明，在光激活后，ATR可以连续释放并重新结合到任何保留在活性样构象中的受体上。和其他人一样

更新日期：2016-10-20

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