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)

Abstract

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 www.springerlink.com
• Keywords: G protein coupled receptor, fluorescence resonance energy transfer, time-resolved fluorescence resonance energy transfer, bioluminescence resonance energy transfer, high throughput, arrestin, drug discovery
• Status: Published
• Refereed: Yes
• 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
• Publisher: Springer
• ISSN: 1618-2642
• ISSN (Online): 1618-2650
• Published Online: 02 June 2010
• Copyright Holders: Copyright © 2010 Springer

Related URLs

• PubMed

Project Code	Award No	Project Name	Principal Investigator	Funder's Name	Funder Ref	Lead Dept
43705	1	Exploring the selectivity and consequences of GPCR homo and hetero dimerisation/oligomerisation using receptors activated solely by ......	Graeme Milligan	Biotechnology and Biological Sciences Research Council (BBSRC)	BB/E006302/1	Institute of Neuroscience and Psychology
51063	1	The organisational structure of class A GPCRs: implications for function and drug design	Graeme Milligan	Medical Research Council (MRC)	G0900050	Institute of Neuroscience and Psychology