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TRPV3 in Drug Development
Lisa M Broad1, Adrian J Mogg2, Elizabeth Eberle3
1Lilly Research Centre, Eli Lilly and Company Ltd., Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK. broad_lisa@lilly.com.
Pharmaceuticals (Basel, Switzerland)
|September 13, 2016
Summary
Transient Receptor Potential Vanilloid 3 (TRPV3) channels in the skin are key to sensing temperature and pain. Research highlights their role in skin conditions, suggesting TRPV3 antagonists as potential treatments.
Area of Science:
- Molecular Biology
- Dermatology
- Neuroscience
Background:
- Transient Receptor Potential Vanilloid 3 (TRPV3) is a thermo-TRP channel highly expressed in the skin.
- TRPV3 plays a significant role in skin physiology, pathophysiology, thermo-sensing, and nociception.
- Genetic studies, including gain-of-function mutations in humans and rodents, have elucidated TRPV3's function in skin health and disease.
Purpose of the Study:
- To explore the role and therapeutic potential of TRPV3 channels.
- To investigate the implications of TRPV3 in skin conditions, itch, and pain.
- To review the current status of TRPV3-targeted therapeutics.
Main Methods:
- Genetic analysis (mutations, knock-outs).
- Pharmacological studies using selective tools.
- Review of pre-clinical and clinical data.
Main Results:
- Gain-of-function TRPV3 mutations are linked to specific skin phenotypes.
- Pre-clinical data support TRPV3 antagonists for inflammatory skin conditions, itch, and pain.
- Only one TRPV3 antagonist (GRC15300) has entered clinical trials; no ongoing clinical trials currently exist for TRPV3 antagonists.
Conclusions:
- TRPV3 is a promising therapeutic target for various skin disorders.
- Further clinical investigation of TRPV3 antagonists is warranted.
- Development of TRPV3-blocking compounds could offer new treatment options for skin-related conditions.
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