title: Dynamics of apelin receptor/G protein coupling in living cells.
abstract: During our research on apelin receptor (APJ) signalling in living cells with BRET and FRET, we demonstrated that apelin-13 stimulation can lead to the activation of Gαi2 or Gαi3 through undergoing a molecular rearrangement rather than dissociation in HEK293 cells expressing APJ. Furthermore, Gαo and Gαq also showed involvement in APJ activation through a classical dissociation model. However, both FRET signal and BRET ratio between fluorescent Gαi1 subunit and Gβγ subunits demonstrated little change after apelin-13 stimulation. These results demonstrated that stimulation of APJ with apelin-13 causes activation of Gαi2, Gαi3, Gαo, Gαq; among which Gαi2, Gαi3 were activated through a novel rearrangement process. These results provide helpful data for understanding APJ mediated G-protein signalling.
authors.affiliation: Neurobiology Institute, Jining Medical University, Jining 272067, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Bai
authors.affiliation: Neurobiology Institute, Jining Medical University, Jining 272067, PR China.
authors.forename: Yunlu
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: Neurobiology Institute, Jining Medical University, Jining 272067, PR China.
authors.forename: Xin
authors.initials: X
authors.lastname: Cai
authors.affiliation: Neurobiology Institute, Jining Medical University, Jining 272067, PR China; Division of Metabolic and Vascular Health, Warwick Medical School, University of Warwick, Coventry, UK. Electronic address: Jing.Chen@warwick.ac.uk.
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
mesh_terms: D000075244:Apelin Receptors; D002460:Cell Line; D057809:HEK293 Cells; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000378:metabolism; D021122:Protein Subunits / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: C104575:APLNR protein, human; D000075244:Apelin Receptors; D036341:Intercellular Signaling Peptides and Proteins; D021122:Protein Subunits; D043562:Receptors, G-Protein-Coupled; C495199:apelin-13 peptide
keywords: Apelin receptor; G protein subunit; G protein-coupled receptor; Resonance energy transfer