Target intelligence / Profile preview

Transient receptor potential cation channel subfamily A member 1 and Transient receptor potential cation channel subfamily V member 3 (TRPA1 and TRPV3)

Target
TRPA1 and TRPV3
Molecular classification
Ion channel, Receptor, Transient receptor potential (TRP) channel family
01

Overview

Transient receptor potential cation channel subfamily A member 1 (TRPA1) and Transient receptor potential cation channel subfamily V member 3 (TRPV3) are non-selective cation channels belonging to the TRP superfamily that play essential roles in sensory transduction and tissue homeostasis. TRPA1 is primarily expressed in nociceptive sensory neurons and serves as a molecular sensor for environmental irritants, noxious cold, and endogenous inflammatory mediators, contributing significantly to pain, itch, and respiratory inflammation. TRPV3 is most abundantly expressed in epidermal keratinocytes, where it acts as a sensor for warm temperatures and a regulator of skin barrier formation, wound healing, and hair follicle development. These channels often function in a coordinated manner, particularly in the skin, where TRPV3 activation in keratinocytes can lead to the release of pruritogenic factors that subsequently activate TRPA1 on sensory nerve endings. Both channels are prominent therapeutic targets for chronic inflammatory and sensory disorders; TRPA1 is a focus for neuropathic pain and asthma, while TRPV3 is investigated for treating pruritus and dermatological conditions such as atopic dermatitis and Olmsted syndrome. Pharmacological inhibition of these channels aims to block the influx of calcium and sodium ions, thereby dampening the signaling cascades that lead to pathological pain and itch sensations.

Other names
ANKTM1Transient receptor potential ankyrin 1Wasabi receptorVRL3Transient receptor potential vanilloid 3
02

Mechanism of action

Antagonism of cation influx through the channel pore, preventing neuronal depolarization and inflammatory mediator release.

03

Biological functions

Sensory perceptionNociceptionThermoreceptionPruriceptionSkin homeostasisHair follicle morphogenesis
04

Disease associations

Chronic painNeuropathic painPruritusAtopic dermatitisOlmsted syndromeAsthmaChronic obstructive pulmonary disease (COPD)
05

Safety considerations

Altered thermal sensitivityLoss of protective pain sensationPotential skin barrier disruptionHair growth changes
06

Interacting drugs

HC-030031

8 more in the full profile.

07

Biomarkers

TRPV3 expression in keratinocytesTRPA1 expression in dorsal root gangliaIL-31 levelsTSLP levels

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