Src phosphorylation of micro-receptor is responsible for the receptor switching from an inhibitory to a stimulatory signal.

ABSTRACT: Recent studies have revealed that in G protein-coupled receptor signalings switching between G protein- and beta-arrestin (betaArr)-dependent pathways occurs. In the case of opioid receptors, the signal is switched from the initial inhibition of adenylyl cyclase (AC) to an increase in AC activity (AC activation) during prolonged agonist treatment. The mechanism of such AC activation has been suggested to involve the switching of G proteins activated by the receptor, phosphorylation of signaling molecules, or receptor-dependent recruitment of cellular proteins. Using protein kinase inhibitors, dominant negative mutant studies and mouse embryonic fibroblast cells isolated from Src kinase knock-out mice, we demonstrated that mu-opioid receptor (OPRM1)-mediated AC activation requires direct as

SUBMITTER: Zhang L 

PROVIDER: S-EPMC2629085 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature