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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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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1725018714371260416 |