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Lipids as regulators of the activity of transient receptor potential type V1 (TRPV1) channels.

Abstract：

:After 7 years from its cloning, the transient receptor potential vanilloid type-1 (TRPV1) channel remains the sole membrane receptor mediating the pharmacological effects of the hot chilli pepper pungent component, capsaicin, and of the Euphorbia toxin, resiniferatoxin. Yet, this ion channel represents one of the most complex examples of how the activity of a protein can be regulated. Among the several chemicophysical stimuli that can modulate TRPV1 permeability to cations, endogenous lipids appear to play a major role, either as allosteric effectors or as direct agonists, or both. Furthermore, the capability of some mediators, such as the endocannabinoid anandamide, or the eicosanoid precursors 12- and 5-hydroperoxy-eicosatetraenoic acids, to activate TRPV1 receptors provides a striking example of the "site-dependent" and "metabolic" functional plasticity, respectively, typical of bioactive lipids. In this article, the multi-faceted and most recently discovered aspects of TRPV1 regulation are reviewed, with particular emphasis on the interaction between these membrane channels and some lipid molecules.

journal_name

Life Sci

journal_title

Life sciences

authors

De Petrocellis L,Di Marzo V

doi

10.1016/j.lfs.2005.05.021

subject

Has Abstract

pub_date

2005-08-19 00:00:00

pages

1651-66

issue

14

eissn

0024-3205

issn

1879-0631

pii

S0024-3205(05)00488-1

journal_volume

77

pub_type

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