Applications of fluorescence and bioluminescence resonance energy transfer to drug discovery at G protein coupled receptors

Alvarez-Curto, E. , Pediani, J. D. and Milligan, G. (2010) Applications of fluorescence and bioluminescence resonance energy transfer to drug discovery at G protein coupled receptors. Analytical and Bioanalytical Chemistry, 398(1), pp. 167-180. (doi: 10.1007/s00216-010-3823-4) (PMID:20517598)

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The role of G protein coupled receptors (GPCRs) in numerous physiological processes that may be disrupted or modified in disease makes them key targets for the development of new therapeutic medicines. A wide variety of resonance energy transfer (RET) techniques such as fluorescence RET and bioluminescence RET have been developed in recent years to detect protein–protein interactions in living cells. Furthermore, these techniques are now being exploited to screen for novel compounds that activate or block GPCRs and to search for new, previously undiscovered signaling pathways activated by well-known pharmacologically classified drugs. The high resolution that can be achieved with these RET methods means that they are well suited to study both intramolecular conformational changes in response to ligand binding at the receptor level and intermolecular interactions involving protein translocation in subcellular compartments resulting from external stimuli. In this review we highlight the latest advances in these technologies to illustrate general principles.

Item Type:Articles
Additional Information:The original publication is available at
Keywords:G protein coupled receptor, fluorescence resonance energy transfer, time-resolved fluorescence resonance energy transfer, bioluminescence resonance energy transfer, high throughput, arrestin, drug discovery
Glasgow Author(s) Enlighten ID:Pediani, Dr John and Alvarez-Curto, Dr Elisa and Milligan, Professor Graeme
Authors: Alvarez-Curto, E., Pediani, J. D., and Milligan, G.
Subjects:Q Science > QH Natural history > QH345 Biochemistry
College/School:College of Medical Veterinary and Life Sciences > School of Psychology & Neuroscience
Journal Name:Analytical and Bioanalytical Chemistry
ISSN (Online):1618-2650
Published Online:02 June 2010
Copyright Holders:Copyright © 2010 Springer
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Project CodeAward NoProject NamePrincipal InvestigatorFunder's NameFunder RefLead Dept
437051Exploring the selectivity and consequences of GPCR homo and hetero dimerisation/oligomerisation using receptors activated solely by ......Graeme MilliganBiotechnology and Biological Sciences Research Council (BBSRC)BB/E006302/1Institute of Neuroscience and Psychology
510631The organisational structure of class A GPCRs: implications for function and drug designGraeme MilliganMedical Research Council (MRC)G0900050Institute of Neuroscience and Psychology