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Intramolecular and Intermolecular FRET Sensors for GPCRs – Monitoring Conformational Changes and Beyond
Trends in Pharmacological Sciences ( IF 13.9 ) Pub Date : 2017-11-25 , DOI: 10.1016/j.tips.2017.10.011
Michael Kauk , Carsten Hoffmann

Within the past decade, a large increase in structural knowledge from crystallographic studies has significantly fostered our understanding of the structural biology of G protein-coupled receptors (GPCRs). However, information on dynamic events upon receptor activation or deactivation is not yet readily accessed by these structural approaches. GPCR-based fluorescence resonance energy transfer or bioluminescence resonance energy transfer sensors or sensors for interacting proteins (e.g., G proteins or arrestins) can in part cover this gap. The principal design of such sensors was reported 15 years ago. Since then, sensors for almost 20 different GPCRs have been designed. If used with necessary controls and cautious interpretation, such sensors can contribute significantly to our understanding of the basic mechanisms of GPCR function and beyond. In this review, we will discuss the recent developments in this area of GPCR dynamics.



中文翻译:

用于GPCR的分子内和分子间FRET传感器–监测构象变化及其他

在过去的十年中,晶体学研究中对结构知识的大量增加极大地促进了我们对G蛋白偶联受体(GPCR)的结构生物学的理解。然而,这些结构方法尚不容易获得有关受体激活或失活后动态事件的信息。基于GPCR的荧光共振能量转移或生物发光共振能量转移传感器或用于相互作用的蛋白质(例如G蛋白或抑制蛋白)的传感器可以部分弥补这一差距。这种传感器的主要设计是在15年前报道的。从那时起,已经设计出了将近20种不同的GPCR的传感器。如果与必要的控件和谨慎的解释一起使用,则此类传感器可以极大地帮助我们理解GPCR功能及其以外的基本机制。

更新日期:2017-11-25
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