Ligand-induced activation of ERK1/2 signaling by constitutively active Gs-coupled 5-HT receptors.

In this study, we investigated these two signaling pathways originating from the three Gs-coupled 5-HT receptors in AD293 cells. We found that the phosphorylation and activation of ERK1/2 are ligand-induced, in contrast to the constitutively active Gs signaling. This indicates that Gs signaling alone is not sufficient for ERK1/2 activation in these three 5-HT receptors. In addition to Gs, we found that β-arrestin and Fyn are essential for the activation of ERK1/2. Together, these results put forth a novel mechanism for ERK1/2 activation involving the cooperative action of Gs, β-arrestin, and Fyn.
PMID: 30833707 [PubMed - as supplied by publisher]

Source: Acta Pharmacologica Sinica - March 3, 2019 Category: Drugs & Pharmacology Authors: Liu P, Yin YL, Wang T, Hou L, Wang XX, Wang M, Zhao GG, Shi Y, Xu HE, Jiang Y Tags: Acta Pharmacol Sin Source Type: research