Asymmetrical ligand-induced cross-regulation of chemokine (C-X-C motif) receptor 4 by α₁-adrenergic receptors at the heteromeric receptor complex.

ABSTRACT: Recently, we reported that chemokine (C-X-C motif) receptor (CXCR)4 and atypical chemokine receptor 3 regulate α₁-adrenergic receptors (α₁-AR) through the formation of hetero-oligomeric complexes. Whether α₁-ARs also regulate chemokine receptor function within such heteromeric receptor complexes is unknown. We observed that activation of α_1b-AR within the α_1b-AR:CXCR4 heteromeric complex leads to cross-recruitment of β-arrestin2 to CXCR4, which could not be inhibited with AMD3100. Activation of CXCR4 did not cross-recruit β-arrestin2 to α_1b-AR. A peptide analogue of transmembrane domain 2 of CXCR4 interfered with α_1b-AR:CXCR4 heteromerization and inhibited α_1b-AR-mediated β-arrestin2 cross-recruitment.

SUBMITTER: Gao X 

PROVIDER: S-EPMC5807542 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature