Agonists and protein kinase C-activation induce phosphorylation and internalization of FFA1 receptors.

Abstract:

:FFA1 (previously known as GPR40) is a free fatty acid receptor involved in the regulation of inflammatory processes and insulin secretion. The cellular actions resulting from FFA1 activation have received considerable attention. However, little is known on the regulation of the receptor function. In the present work, using cells transfected with this receptor, docosahexaenoic acid and α-linolenic acid increased intracellular calcium concentration and ERK 1/2 phosphorylation. It was also observed that FFA1 is a phosphoprotein whose phosphorylation state was increased (2- to 3-fold) by agonists (i.e., free fatty acids) and also by phorbol myristate acetate. Agonist- and phorbol ester-mediated FFA1 phosphorylation was markedly reduced by inhibitors of protein kinase C. Receptor stimulation by free fatty acids and protein kinase C activation also induced receptor internalization as evidenced by confocal microscopy. In summary, our data show that FFA1 is a phosphoprotein whose phosphorylation state is modulated by agonists and protein kinase C activation; such covalent modification is associated with receptor internalization.

journal_name

Eur J Pharmacol

authors

Sosa-Alvarado C,Hernández-Méndez A,Romero-Ávila MT,Sánchez-Reyes OB,Takei Y,Tsujimoto G,Hirasawa A,García-Sáinz JA

doi

10.1016/j.ejphar.2015.10.038

subject

Has Abstract

pub_date

2015-12-05 00:00:00

pages

108-15

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(15)30318-6

journal_volume

768

pub_type

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