TRPV1: A Target for Rational Drug Design

Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ 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 c...

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Main Authors: Vincenzo Carnevale, Tibor Rohacs
Format: Article
Language:English
Published: MDPI AG 2016-08-01
Series:Pharmaceuticals
Subjects:
Online Access:http://www.mdpi.com/1424-8247/9/3/52
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spelling doaj-20731acc3dee452b804ed02794bd4d4c2020-11-25T01:46:33ZengMDPI AGPharmaceuticals1424-82472016-08-01935210.3390/ph9030052ph9030052TRPV1: A Target for Rational Drug DesignVincenzo Carnevale0Tibor Rohacs1Institute for Computational Molecular Science, Temple University, Philadelphia, PA 19122, USANew Jersey Medical School, Rutgers University, Newark, NJ 07103, USATransient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ 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.http://www.mdpi.com/1424-8247/9/3/52TRPV1capsaicinvanilloidpainnociception
collection DOAJ
language English
format Article
sources DOAJ
author Vincenzo Carnevale
Tibor Rohacs
spellingShingle Vincenzo Carnevale
Tibor Rohacs
TRPV1: A Target for Rational Drug Design
Pharmaceuticals
TRPV1
capsaicin
vanilloid
pain
nociception
author_facet Vincenzo Carnevale
Tibor Rohacs
author_sort Vincenzo Carnevale
title TRPV1: A Target for Rational Drug Design
title_short 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_sort trpv1: a target for rational drug design
publisher MDPI AG
series Pharmaceuticals
issn 1424-8247
publishDate 2016-08-01
description Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ 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.
topic TRPV1
capsaicin
vanilloid
pain
nociception
url http://www.mdpi.com/1424-8247/9/3/52
work_keys_str_mv AT vincenzocarnevale trpv1atargetforrationaldrugdesign
AT tiborrohacs trpv1atargetforrationaldrugdesign
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