TRPV1: A target for rational drug design

Vincenzo Carnevale, Tibor Rohacs

Research output: Contribution to journalReview articlepeer-review

65 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 languageEnglish (US)
Article number52
JournalPharmaceuticals
Volume9
Issue number3
DOIs
StatePublished - 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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