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Abstract Title:

Thimerosal decreases TRPV1 activity by oxidation of extracellular sulfhydryl residues.

Abstract Source:

Neurosci Lett. 2004 Oct 21 ;369(3):250-5. PMID: 15464274

Abstract Author(s):

Yunju Jin, Dong Kwan Kim, Lee-Yong Khil, Uhtaek Oh, Jun Kim, Jiyeon Kwak

Article Affiliation:

Yunju Jin

Abstract:

TRPV1, a receptor for capsaicin, plays a key role in mediating thermal and inflammatory pain. Because the modulation of ion channels by the cellular redox state is a significant determinant of channel function, we investigated the effects of sulfhydryl modification on the activity of TRPV1. Thimerosal, which oxidizes sulfhydryls, blocked the capsaicin-activated inward current (I(cap)) in cultured sensory neurons, in a reversible and dose-dependent manner, which was prevented by the co-application of the reducing agent, dithiothreitol. Among the three cysteine residues of TRPV1 that are exposed to the extracellular space, the oxidation-induced effect of thimerosal on I(cap) was blocked only by a point mutation at Cys621. These results suggest that the modification of an extracellular thiol group can alter the activity of TRPV1. Consequently, we propose that such a modulation of the redox state might regulate the physiological activity of TRPV1.

Study Type : In Vitro Study
Additional Links
Problem Substances : Thimerosal : CK(799) : AC(190)

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Sayer Ji
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