4-Hydroxynonenal-induced GPR109A (HCA₂ receptor) activation elicits bipolar responses, G_αi -mediated anti-inflammatory effects and G_βγ -mediated cell death.

ABSTRACT:

Background and purpose

In this study, we examined the possibility that 4-hydroxynonenal (4-HNE) acting as a ligand for the HCA₂ receptor (GPR109A) elicits both anti-inflammatory and cell death responses.

Experimental approach

Agonistic activity of 4-HNE was determined by observing the inhibition of cAMP generation in CHO-K1-GPR109A-G_i cell line, using surface plasmon resonance (SPR) binding and competition binding assays with [³ H]-niacin. 4-HNE-mediated signalling pathways and cellular responses were investigated in cells expressing GPR109A and those not expressing these receptors.

Key results

Agonistic activity of 4-HNE was stronger than that of niacin or 3-OHBA at inhibiting forskolin-induced cAMP production and SPR binding affinity

SUBMITTER: Gautam J 

PROVIDER: S-EPMC6003634 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature