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TRPV1: A Target for Rational Drug Design

Vincenzo Carnevale1, Tibor Rohacs2

  • 1Institute for Computational Molecular Science, Temple University, Philadelphia, PA 19122, USA. vincenzo.carnevale@temple.edu.

Pharmaceuticals (Basel, Switzerland)
|August 27, 2016
PubMed

Insights

Transient Receptor Potential Vanilloid 1 (TRPV1) channels are key targets for pain relief. This review explores TRPV1 antagonists and agonists, discussing strategies for developing improved drugs using new structural data.

Area of Science:

  • Molecular biology
  • Neuroscience
  • Pharmacology

Background:

  • Transient Receptor Potential Vanilloid 1 (TRPV1) is a Ca(2+) permeable cation channel activated by heat and chemicals like capsaicin.
  • TRPV1 plays a significant role in pain signaling pathways.
  • Existing TRPV1-targeting drugs have not reached routine clinical use.

Purpose of the Study:

  • To review the therapeutic potential of TRPV1 antagonists and agonists for pain management.
  • To discuss strategies for developing novel and improved TRPV1-targeting drugs.
  • To leverage recent high-resolution structural data of TRPV1 for drug design.

Main Methods:

  • Literature review of existing research on TRPV1.
  • Analysis of high-resolution structural data of the TRPV1 channel.
  • Discussion of drug development strategies for TRPV1 modulators.

Main Results:

  • Numerous compounds targeting TRPV1 have been developed, but none are in widespread clinical use.
  • High-resolution structures provide new insights into TRPV1 channel function and drug binding.
  • Both antagonists and agonists show potential for therapeutic applications beyond pain.

Conclusions:

  • TRPV1 remains a promising target for novel therapeutics.
  • Utilizing structural biology is crucial for designing more effective and selective TRPV1 drugs.
  • Further research is needed to overcome challenges in clinical translation for TRPV1-based therapies.
Keywords:
TRPV1capsaicinnociceptionpainvanilloid

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