Transactivation of G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs): Recent insights using luminescence and fluorescence technologies.
Curr Opin Endocr Metab Res
; 16: 102-112, 2021 Feb.
Article
in En
| MEDLINE
| ID: mdl-33748531
ABSTRACT
Alterations in signalling due to bidirectional transactivation of G protein-coupled receptor (GPCRs) and receptor tyrosine kinases (RTKs) are well established. Transactivation significantly diversifies signalling networks within a cell and has been implicated in promoting both advantageous and disadvantageous physiological and pathophysiological outcomes, making the GPCR/RTK interactions attractive new targets for drug discovery programmes. Transactivation has been observed for a plethora of receptor pairings in multiple cell types; however, the precise molecular mechanisms and signalling effectors involved can vary with receptor pairings and cell type. This short review will discuss the recent applications of proximity-based assays, such as resonance energy transfer and fluorescence-based imaging in investigating the dynamics of GPCR/RTK complex formation, subsequent effector protein recruitment and the cellular locations of complexes in living cells.
5-hydroxytryptamine receptor 1A, (5-HT1A); Endocytosis; Förster Resonance Energy Transfer, (FRET); G protein-coupled receptor; G protein-coupled receptors, (GPCRs); GPCR kinases, (GRKs); Oligomeric complexes; Receptor tyrosine kinase; Resonance energy transfer; Transactivation; adrenoceptors, (AR); bioluminescence resonance energy transfer, (BRET); cannabinoid receptor 2, (CB2R); disintegrin and metalloproteinases, (ADAMs); epidermal growth factor receptor, (EGFR); epidermal growth factor, (EGF); fibroblast growth factor receptor, (FGFR); fluorescence correlation spectroscopy, (FCS); formyl peptide receptor, (FPR); free fatty acid, (FFA); heparin binding EGF, (Hb-EGF); hepatocyte growth factor, (HGF); human umbilical vein endothelial cells, (HUVECs); insulin growth factor receptor-1, (IGFR-1); insulin receptor, (IR); lysophosphatidic acid receptor 1, (LPA); matrix metalloproteinases, (MMPs); platelet-derived growth factor receptor, (PDGFR); proximity ligation assay, (PLA); reactive oxygen species, (ROS); receptor tyrosine kinases, (RTKs); sphingosine-1-phosphate receptor, (S1PR); tetrahydrocannabinol, (THC); total internal reflection fluorescence microscopy, (TIRF-M); vascular endothelial growth factor receptor 2, (VEGFR2); vascular endothelial growth factor, (VEGF); vasopressin 2 receptor, (V2R)
Full text:
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Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
Curr Opin Endocr Metab Res
Year:
2021
Document type:
Article
Affiliation country:
Reino Unido