PMID- 21864280
OWN - NLM
STAT- MEDLINE
DCOM- 20120228
LR  - 20190823
IS  - 1875-533X (Electronic)
IS  - 0929-8673 (Linking)
VI  - 18
IP  - 30
DP  - 2011
TI  - Oligomerization of G protein-coupled receptors: biochemical and biophysical 
      methods.
PG  - 4606-34
AB  - Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed 
      almost 30 years ago, have crucial relevance for drug design. Indeed, formation of 
      GPCR oligomers may affect the diversity and performance by which extracellular 
      signals are transferred to G proteins in the process of receptor transduction. 
      Thus, the control of oligomer assembly/disassembly and signaling will be a 
      powerful pharmacological tool. This, however, requires (i) the determination that 
      oligomerization takes place between particular receptors, (ii) the confirmation 
      that the oligomer has pharmacological importance and (iii) the availability of 
      the oligomer 3D structure. This review aims at presenting experimental methods 
      which unveil the complexity of GPCR dimerization/oligomerization focusing on 
      biochemical and biophysical approaches. In total, we review 22 methods, including 
      biochemical methods (radiation inactivation technique, receptor co-expression and 
      trans-complementation studies, cross-linking experiments, co-immunoprecipitation 
      and immunoblotting studies and analysis of receptor mutants and chimeras) and 
      biophysical methods (Fluorescence Resonance Energy Transfer, (FRET), including 
      photobleaching FRET (pb-FRET) and Time-Resolved FRET (TR-FRET), Luminescence 
      Resonance Energy Transfer (LRET), Bioluminescence Resonance Energy Transfer 
      (BRET), Bimolecular Fluorescence Complementation (BiFC), Luminescence 
      Fluorescence Complementation (BiLC), Fluorescence Recovery after Photobleaching 
      (FRAP), Confocal Microscopy, Immunofluorescence Microscopy, Single 
      Fluorescent-Molecule Imaging, Transmission Electron Microscopy, Immunoelectron 
      Microscopy, Atomic Force Microscopy, Total Internal Reflectance Fluorescence 
      Microscopy (TIRFM) and X-ray Crystallography). For each method the scientific 
      basis of the approach is shortly described followed by the extensive description 
      of its application for studying GPCR oligomers presented according to their 
      classes and families. Based on the wealth of experimental evidence, there is no 
      doubt about the existence of GPCR dimers, oligomers and receptor mosaics which 
      constitute a new and highly promising group of novel drug targets for more 
      selective and safer drugs.
FAU - Kaczor, A A
AU  - Kaczor AA
AD  - Research Program on Biomedical Informatics (GRIB), IMIM/Pompeu Fabra University, 
      Barcelona, Spain. agnieszka.kaczor@umlub.pl
FAU - Selent, J
AU  - Selent J
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - United Arab Emirates
TA  - Curr Med Chem
JT  - Current medicinal chemistry
JID - 9440157
RN  - 0 (Cross-Linking Reagents)
RN  - 0 (Receptors, G-Protein-Coupled)
RN  - 0 (Recombinant Fusion Proteins)
RN  - EC 3.6.1.- (GTP-Binding Proteins)
SB  - IM
MH  - Cross-Linking Reagents/chemistry
MH  - Crystallography, X-Ray
MH  - Drug Design
MH  - Fluorescence Resonance Energy Transfer/methods
MH  - GTP-Binding Proteins/chemistry
MH  - Immunoprecipitation
MH  - Luminescence
MH  - Luminescent Measurements
MH  - Microscopy, Atomic Force
MH  - Microscopy, Electron, Transmission
MH  - Microscopy, Fluorescence/methods
MH  - Mutation
MH  - Photobleaching
MH  - *Protein Multimerization
MH  - Receptors, G-Protein-Coupled/*chemistry/genetics/radiation effects
MH  - Recombinant Fusion Proteins
EDAT- 2011/08/26 06:00
MHDA- 2012/03/01 06:00
CRDT- 2011/08/26 06:00
PHST- 2011/06/15 00:00 [received]
PHST- 2011/08/15 00:00 [revised]
PHST- 2011/08/18 00:00 [accepted]
PHST- 2011/08/26 06:00 [entrez]
PHST- 2011/08/26 06:00 [pubmed]
PHST- 2012/03/01 06:00 [medline]
AID - BSP/CMC/E-Pub/2011/ 344 [pii]
AID - 10.2174/092986711797379285 [doi]
PST - ppublish
SO  - Curr Med Chem. 2011;18(30):4606-34. doi: 10.2174/092986711797379285.