Stimulation of TRPV1 channels activates the AP-1 transcription factor.

Stimulation of TRPV1 channels activates the AP-1 transcription factor. Biochem Pharmacol. 2018 Feb 13;: Authors: Backes TM, Rössler OG, Hui X, Grötzinger C, Lipp P, Thiel G Abstract Transient receptor potential vanilloid 1 (TRPV1) channels were originally described as the receptors of capsaicin, the main constituent of hot chili pepper. The biological functions of TRPV1 channels include pain sensation and inflammatory thermal hyperalgesia. Here, we show that stimulation of HEK293 cells expressing TRPV1 channels (H2C1 cells) with capsaicin or the TRPV1 ligand resiniferatoxin activated transcription mediated by the transcription factor AP-1. No cell death was occurring under these experimental conditions. The AP-1 activity was not altered in capsaicin or resiniferatoxin-stimulated HEK293 cells lacking TRPV1. We identified the AP-1 DNA binding site as the capsaicin/resiniferatoxin-responsive element. Stimulation with the TRPV1 ligand N-arachidonoyldopamine increased AP-1 activity in a TRPV1-dependent and TRPV1-independent manner. Stimulation of TRPV1 channels induced an influx of Ca2+ into the cells and this rise in intracellular Ca2+ was essential for activating AP-1 in capsaicin or resiniferatoxin-stimulated cells. N-arachidonoyldopamine stimulation induced a rise in intracellular Ca2+ in a TRPV-1 dependent and independent manner. AP-1 is a dimeric transcription factor, composed of proteins of the c-Jun, c-Fos and ATF families. Stim...
Source: Biochemical Pharmacology - Category: Drugs & Pharmacology Authors: Tags: Biochem Pharmacol Source Type: research