TRPV1: A target for rational drug design

Vincenzo Carnevale; Tibor Rohacs

doi:10.3390/ph9030052

TRPV1: A target for rational drug design

Vincenzo Carnevale, Tibor Rohacs

Research output: Contribution to journal › Review article › peer-review

75 Scopus citations

Abstract

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.

Original language	English (US)
Article number	52
Journal	Pharmaceuticals
Volume	9
Issue number	3
DOIs	https://doi.org/10.3390/ph9030052
State	Published - Sep 23 2016

All Science Journal Classification (ASJC) codes

Molecular Medicine
Pharmaceutical Science
Drug Discovery

Keywords

Capsaicin
Nociception
Pain
TRPV1
Vanilloid

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10.3390/ph9030052

Cite this

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title = "TRPV1: A target for rational drug design",

abstract = "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.",

keywords = "Capsaicin, Nociception, Pain, TRPV1, Vanilloid",

author = "Vincenzo Carnevale and Tibor Rohacs",

note = "Funding Information: Research in the authors{\textquoteright} laboratories were funded by National Science Foundation Grants ACI-1440059 (to V.C.) and NIH Grants R01NS055159 and R01GM093290 (to T.R.). Publisher Copyright: {\textcopyright} 2016 by the authors; licensee MDPI, Basel, Switzerland.",

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AU - Rohacs, Tibor

N1 - Funding Information: Research in the authors’ laboratories were funded by National Science Foundation Grants ACI-1440059 (to V.C.) and NIH Grants R01NS055159 and R01GM093290 (to T.R.). Publisher Copyright: © 2016 by the authors; licensee MDPI, Basel, Switzerland.

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N2 - 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.

AB - 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.

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KW - Vanilloid

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TRPV1: A target for rational drug design

Abstract

All Science Journal Classification (ASJC) codes

Keywords

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