Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 39, Issue 2, Pages 123-135Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2017.10.011
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Funding
- Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) [TRR 166]
- Marie Curie Initial Training Networks (ITN) [608180]
- international doctoral college 'Receptor Dynamics: Emerging Paradigms for Novel Drugs' fund
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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.
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