20-Hydroxyeicosatetraenoic acid (20-HETE) is a novel activator of transient receptor potential vanilloid 1 (TRPV1) channel

Hairuo Wen, Johan Östman, Kristen J. Bubb, Catherine Panayiotou, John V. Priestley, Mark D. Baker, Amrita Ahluwalia

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48 Citations (Scopus)

Abstract

TRPV1 is a member of the transient receptor potential ion channel family and is gated by capsaicin, the pungent component of chili pepper. It is expressed predominantly in small diameter peripheral nerve fibers and is activated by noxious temperatures >42°C. 20-Hydroxyeicosatetraenoic acid (20-HETE) is a cytochrome P-450 4A/4F-derived metabolite of the membrane phospholipid arachidonic acid. It is a powerful vasoconstrictor and has structural similarities with other TRPV1 agonists, e.g. the hydroperoxyeicosatetraenoic acid 12-HPETE, and we hypothesized that it may be an endogenous ligand for TRPV1 in sensory neurons innervating the vasculature. Here, we demonstrate that 20-HETE both activates and sensitizes mouse and human TRPV1, in a kinase-dependent manner, involving the residue Ser 502 in heterologously expressed hTRPV1, at physiologically relevant concentrations.

Original languageEnglish
Pages (from-to)13868-13876
Number of pages9
JournalJournal of Biological Chemistry
Volume287
Issue number17
DOIs
Publication statusPublished - 20 Apr 2012
Externally publishedYes

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