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Biosci Rep. 2017 Apr 20;37(2). pii: BSR20160547. doi: 10.1042/BSR20160547. Print 2017 Apr 30.

Methods used to study the oligomeric structure of G-protein-coupled receptors.

Author information

1
Faculty of Environmental Science and Engineering, Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, Yunnan, China.
2
First People's Hospital of Yunnan Province, Kunming, Yunnan, China.
3
Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, U.K.
4
Faculty of Environmental Science and Engineering, Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, Yunnan, China tianruixu@kmust.edu.cn.

Abstract

G-protein-coupled receptors (GPCRs), which constitute the largest family of cell surface receptors, were originally thought to function as monomers, but are now recognized as being able to act in a wide range of oligomeric states and indeed, it is known that the oligomerization state of a GPCR can modulate its pharmacology and function. A number of experimental techniques have been devised to study GPCR oligomerization including those based upon traditional biochemistry such as blue-native PAGE (BN-PAGE), co-immunoprecipitation (Co-IP) and protein-fragment complementation assays (PCAs), those based upon resonance energy transfer, FRET, time-resolved FRET (TR-FRET), FRET spectrometry and bioluminescence resonance energy transfer (BRET). Those based upon microscopy such as FRAP, total internal reflection fluorescence microscopy (TIRFM), spatial intensity distribution analysis (SpIDA) and various single molecule imaging techniques. Finally with the solution of a growing number of crystal structures, X-ray crystallography must be acknowledged as an important source of discovery in this field. A different, but in many ways complementary approach to the use of more traditional experimental techniques, are those involving computational methods that possess obvious merit in the study of the dynamics of oligomer formation and function. Here, we summarize the latest developments that have been made in the methods used to study GPCR oligomerization and give an overview of their application.

KEYWORDS:

FRET technology; GPCR; computational methods; oligomerization

PMID:
28062602
PMCID:
PMC5398257
DOI:
10.1042/BSR20160547
[Indexed for MEDLINE]
Free PMC Article

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