Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels

Leucettamols, bifunctionalized sphingoid-like compounds obtained from a marine sponge Leucetta sp., act as non-electrophilic activators of the TRPA1 channel and potent inhibitors of the icilin-mediated activation of the TRPM8 channel, while they are inactive on CB1, CB2 and TRPV1 receptors. Leucetta...

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Main Authors:	Chianese, Giuseppina, Fattorusso, Ernesto, Putra, Masteria Yunovilsa, Calcinai, Barbara, Bavestrello, Giorgio, Moriello, Aniello Schiano, Petrocellis, Luciano De, Marzo, Vincenzo Di, Taglialatela-Scafati, Orazio
Format:	Online
Language:	English
Published:	MDPI 2012
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509527/

id	pubmed-3509527
recordtype	oai_dc
spelling	pubmed-35095272012-12-10 Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels Chianese, Giuseppina Fattorusso, Ernesto Putra, Masteria Yunovilsa Calcinai, Barbara Bavestrello, Giorgio Moriello, Aniello Schiano Petrocellis, Luciano De Marzo, Vincenzo Di Taglialatela-Scafati, Orazio Article Leucettamols, bifunctionalized sphingoid-like compounds obtained from a marine sponge Leucetta sp., act as non-electrophilic activators of the TRPA1 channel and potent inhibitors of the icilin-mediated activation of the TRPM8 channel, while they are inactive on CB1, CB2 and TRPV1 receptors. Leucettamols represent the first compounds of marine origin to target TRPA1 and the first class of natural products to inhibit TRPM8 channels. The preparation of a small series of semi-synthetic derivatives revealed interesting details on the structure-activity relationships within this new chemotype of simple acyclic TRP modulators. MDPI 2012-11-02 /pmc/articles/PMC3509527/ /pubmed/23203269 http://dx.doi.org/10.3390/md10112435 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Chianese, Giuseppina Fattorusso, Ernesto Putra, Masteria Yunovilsa Calcinai, Barbara Bavestrello, Giorgio Moriello, Aniello Schiano Petrocellis, Luciano De Marzo, Vincenzo Di Taglialatela-Scafati, Orazio
spellingShingle	Chianese, Giuseppina Fattorusso, Ernesto Putra, Masteria Yunovilsa Calcinai, Barbara Bavestrello, Giorgio Moriello, Aniello Schiano Petrocellis, Luciano De Marzo, Vincenzo Di Taglialatela-Scafati, Orazio Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
author_facet	Chianese, Giuseppina Fattorusso, Ernesto Putra, Masteria Yunovilsa Calcinai, Barbara Bavestrello, Giorgio Moriello, Aniello Schiano Petrocellis, Luciano De Marzo, Vincenzo Di Taglialatela-Scafati, Orazio
author_sort	Chianese, Giuseppina
title	Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
title_short	Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
title_full	Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
title_fullStr	Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
title_full_unstemmed	Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels
title_sort	leucettamols, bifunctionalized marine sphingoids, act as modulators of trpa1 and trpm8 channels
description	Leucettamols, bifunctionalized sphingoid-like compounds obtained from a marine sponge Leucetta sp., act as non-electrophilic activators of the TRPA1 channel and potent inhibitors of the icilin-mediated activation of the TRPM8 channel, while they are inactive on CB1, CB2 and TRPV1 receptors. Leucettamols represent the first compounds of marine origin to target TRPA1 and the first class of natural products to inhibit TRPM8 channels. The preparation of a small series of semi-synthetic derivatives revealed interesting details on the structure-activity relationships within this new chemotype of simple acyclic TRP modulators.
publisher	MDPI
publishDate	2012
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509527/
_version_	1611936403712638976

Leucettamols, Bifunctionalized Marine Sphingoids, Act as Modulators of TRPA1 and TRPM8 Channels

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