| Literature DB >> 33748531 |
Laura E Kilpatrick1,2, Stephen J Hill3,2.
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.Entities:
Keywords: 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)
Year: 2021 PMID： 33748531 PMCID： PMC7960640 DOI： 10.1016/j.coemr.2020.10.003
Source DB: PubMed Journal: Curr Opin Endocr Metab Res ISSN： 2451-9650