TRPV1: A Target for Rational Drug Design

Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca(2+) permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine...

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Detalles Bibliográficos
Autores principales: Carnevale, Vincenzo, Rohacs, Tibor
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5039505/
https://www.ncbi.nlm.nih.gov/pubmed/27563913
http://dx.doi.org/10.3390/ph9030052
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author Carnevale, Vincenzo
Rohacs, Tibor
author_facet Carnevale, Vincenzo
Rohacs, Tibor
author_sort Carnevale, Vincenzo
collection PubMed
description Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca(2+) permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine clinical practice. This review will discuss the rationale for antagonists and agonists of TRPV1 for pain relief and other conditions, and strategies to develop new, better drugs to target this ion channel, using the newly available high-resolution structures.
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spelling pubmed-50395052016-10-04 TRPV1: A Target for Rational Drug Design Carnevale, Vincenzo Rohacs, Tibor Pharmaceuticals (Basel) Review Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca(2+) permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine clinical practice. This review will discuss the rationale for antagonists and agonists of TRPV1 for pain relief and other conditions, and strategies to develop new, better drugs to target this ion channel, using the newly available high-resolution structures. MDPI 2016-08-23 /pmc/articles/PMC5039505/ /pubmed/27563913 http://dx.doi.org/10.3390/ph9030052 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Carnevale, Vincenzo
Rohacs, Tibor
TRPV1: A Target for Rational Drug Design
title TRPV1: A Target for Rational Drug Design
title_full TRPV1: A Target for Rational Drug Design
title_fullStr TRPV1: A Target for Rational Drug Design
title_full_unstemmed TRPV1: A Target for Rational Drug Design
title_short TRPV1: A Target for Rational Drug Design
title_sort trpv1: a target for rational drug design
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5039505/
https://www.ncbi.nlm.nih.gov/pubmed/27563913
http://dx.doi.org/10.3390/ph9030052
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