Role of the Helix-8 and C-Terminal Tail in Regulating Proteinase Activated Receptor 2 Signaling.

ABSTRACT: The C-terminal tail of G-protein-coupled receptors (GPCR) contain important regulatory sites that enable interaction with intracellular signaling effectors. Here we examine the relative contribution of the C-tail serine/threonine phosphorylation sites (Ser^383-385, Ser³⁸⁷-Thr³⁹²) and the helix-8 palmitoylation site (Cys³⁶¹) in signaling regulation downstream of the proteolytically activated GPCR, PAR2. We examined Gα_q/11-coupled calcium signaling, β-arrestin-1/-2 recruitment, and MAPK activation (p44/42 phosphorylation) by wild-type and mutant receptors expressed in a CRISPR/Cas9 PAR2-knockout HEK-293 cell background with both peptide stimulation of the receptor (SLIGRL-NH₂) as well as activation with its endogenous trypsin r

SUBMITTER: Thibeault PE 

PROVIDER: S-EPMC7551709 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature