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Transient receptor potential vanillin 3 (TRPV3) is a member of the transient receptor potential (TRP) superfamily. As a Ca-permeable nonselective cation channel, TRPV3 can recognize thermal stimulation (31-39 °C), and it plays an important regulatory role in temperature perception, pain transduction, skin physiology, inflammation, cancer and other diseases. TRPV3 is not only activated by the changes in the temperature, but it also can be activated by a variety of chemical and physical stimuli. Selective TRPV3 agonists and antagonists with regulatory effects and the physiological functions for clinical application are highly demanded. In recent years, significant progress has been made in the study of TRPV3, but there is still a lack of modulators with a strong affinity and excellent selectivity. This paper reviews the functional characteristics of TRPV3 in terms of the structure, diseases and the research on TRPV3 modulators.
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http://dx.doi.org/10.3390/molecules28020774 | DOI Listing |
The heat-responses of the homotetrameric thermosensitive transient receptor potential vanilloid (TRPV)1-4 channels are use-dependent. The initial short heat stimulus typically alters the temperature threshold and sensitivity for the subsequent one. The precise underlying structural motifs have not been identified except for TRPV1 and TRPV3.
View Article and Find Full Text PDFChem Biodivers
March 2025
NITTE (Deemed to be University), Pharmacology, Nitte Paneer, 30030, Mangalore, INDIA.
Transient Receptor Potential Vanilloid 3 (TRPV3) is a thermosensitive calcium-permeable ion channel and has a function in sensory perception, epidermal barrier function, inflammation, and keratinocyte proliferation. TRPV3 dysfunction is linked with chronic pain, atopic dermatitis, and neurodegenerative disorders. This study compared the binding efficacy and molecular dynamics of cannabidiol- and eugenol- TRPV3 complex(s), elucidating their ligand-protein dynamics.
View Article and Find Full Text PDFBoth hot and cold sensation of the homotetrameric thermosensitive transient receptor potential vanilloid 1-4 (TRPV1-4) channels have been predicted by a single Gibbs-Helmholtz equation for a change in molar heat capacity. However, cold activation has not been confirmed for those heat-responsive TRPV1-4 channels. Given the cooperative heat unfolding and non-cooperative cold unfolding behaviors in proteins, two different open states at low and high temperatures should be detected in TRPV1-4 channels.
View Article and Find Full Text PDFNat Struct Mol Biol
February 2025
Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA.
The transient receptor potential vanilloid 2 (TRPV2) cation channel is a key player in cardiovascular physiology and pathophysiology. Probenecid (PBC), an FDA-approved uricosuric agent thought to activate TRPV2, has shown promise in enhancing cardiovascular function in both preclinical and clinical studies. Here our electrophysiological data reveal that PBC significantly potentiates rat TRPV2 to known stimuli, and cryo electron microscopy structures show that PBC directly interacts with rat TRPV2 in a previously unidentified intracellular binding pocket.
View Article and Find Full Text PDFFront Med (Lausanne)
January 2025
Department of Dermatology, Changzhi People's Hospital, Changzhi, China.
Olmsted syndrome (OS) is a rare disorder characterized by a mutilating palmoplantar keratoderma and periorificial keratotic plaques, but which shows considerable clinical heterogeneity. Recently, transient receptor potential vanilloid 3 () mutations associated with autosomal dominant or recessive OS have been reported. Here we describe a classically OS case with definitive diagnosis of OS based on clinical features and a genetic assay.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!