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Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
12:09

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

TRPV4 agonists and antagonists

Fabien Vincent1, Matthew A J Duncton

  • 1Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), Two Corporate Drive, South San Francisco, CA 94066, USA. fabien_vincent_us@yahoo.com

Current Topics in Medicinal Chemistry
|June 16, 2011
PubMed

Insights

TRPV4 (Transient Receptor Potential Vanilloid 4) ion channels are crucial for various physiological functions. Research is exploring TRPV4 modulators for treating pain, bladder dysfunction, and lung injury.

Area of Science:

  • Ion channel research
  • Physiology
  • Pharmacology

Background:

  • TRPV4 is a polymodal ion channel activated by diverse stimuli like temperature, osmolarity, and lipids.
  • It plays significant roles in skin, kidney, vasculature, and bone.
  • Therapeutic targeting of TRPV4 is gaining interest due to its physiological importance.

Purpose of the Study:

  • To review known small molecule modulators of TRPV4.
  • To discuss progress in identifying potent and selective TRPV4 agonists and antagonists.
  • To highlight therapeutic potential for various conditions.

Main Methods:

  • Review of existing literature on TRPV4 modulators.
  • Analysis of studies using knockout mice and specific agonists (4αPDD, GSK1016790A).
  • Focus on small molecule identification for in vivo interrogation.

Main Results:

  • TRPV4 antagonism is considered for inflammatory and neuropathic pain.
  • TRPV4 modulation may target bladder dysfunctions.
  • Ventilator-induced lung injury is a potential indication for TRPV4 antagonists.

Conclusions:

  • TRPV4 ion channels have diverse physiological roles.
  • Development of selective TRPV4 modulators is advancing.
  • TRPV4 represents a promising therapeutic target for multiple diseases.

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