Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT946IA)

• DTT Name: Transient receptor potential cation channel V3 (TRPV3)
• Synonyms: Vanilloid receptor-like 3; VRL-3; TrpV3
• Gene Name: TRPV3
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Transient receptor potential catioin channel
• UniProt ID: TRPV3_HUMAN
• TTD ID: T58496
• Sequence:
  MKAHPKEMVPLMGKRVAAPSGNPAILPEKRPAEITPTKKSAHFFLEIEGFEPNPTVAKTS
  PPVFSKPMDSNIRQCISGNCDDMDSPQSPQDDVTETPSNPNSPSAQLAKEEQRRKKRRLK
  KRIFAAVSEGCVEELVELLVELQELCRRRHDEDVPDFLMHKLTASDTGKTCLMKALLNIN
  PNTKEIVRILLAFAEENDILGRFINAEYTEEAYEGQTALNIAIERRQGDIAALLIAAGAD
  VNAHAKGAFFNPKYQHEGFYFGETPLALAACTNQPEIVQLLMEHEQTDITSRDSRGNNIL
  HALVTVAEDFKTQNDFVKRMYDMILLRSGNWELETTRNNDGLTPLQLAAKMGKAEILKYI
  LSREIKEKRLRSLSRKFTDWAYGPVSSSLYDLTNVDTTTDNSVLEITVYNTNIDNRHEML
  TLEPLHTLLHMKWKKFAKHMFFLSFCFYFFYNITLTLVSYYRPREEEAIPHPLALTHKMG
  WLQLLGRMFVLIWAMCISVKEGIAIFLLRPSDLQSILSDAWFHFVFFIQAVLVILSVFLY
  LFAYKEYLACLVLAMALGWANMLYYTRGFQSMGMYSVMIQKVILHDVLKFLFVYIVFLLG
  FGVALASLIEKCPKDNKDCSSYGSFSDAVLELFKLTIGLGDLNIQQNSKYPILFLFLLIT
  YVILTFVLLLNMLIALMGETVENVSKESERIWRLQRARTILEFEKMLPEWLRSRFRMGEL
  CKVAEDDFRLCLRINEVKWTEWKTHVSFLNEDPGPVRRTDFNKIQDSSRNNSKTTLNAFE
  EVEEFPETSV
• Function: Putative receptor-activated non-selective calcium permeant cation channel. It is activated by innocuous (warm) temperatures and shows an increased response at noxious temperatures greater than 39 degrees Celsius. Activation exhibits an outward rectification. May associate with TRPV1 and may modulate its activity. Is a negative regulator of hair growth and cycling: TRPV3-coupled signaling suppresses keratinocyte proliferation in hair follicles and induces apoptosis and premature hair follicle regression (catagen).
• KEGG Pathway: Inflammatory mediator regulation of TRP channels (hsa04750)
• Reactome Pathway: TRP channels (R-HSA-3295583)

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SAR292833	DM63QY0	Pain	MG30-MG3Z	Phase 2	[1]

14 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-APB	DM9AKVR	Discovery agent	N.A.	Investigative	[2]
6-tert-butyl-m-cresol	DM9EA3C	Discovery agent	N.A.	Investigative	[3]
aspirin-triggered resolvin D1	DMOP941	Discovery agent	N.A.	Investigative	[4]
borneol	DMWBV1P	Discovery agent	N.A.	Investigative	[3]
carvacrol	DMINM2D	Discovery agent	N.A.	Investigative	[5]
carveol	DMGIZ5U	Discovery agent	N.A.	Investigative	[3]
cinnamaldehyde	DMZDUXG	Discovery agent	N.A.	Investigative	[6]
citral	DM53ZGY	Discovery agent	N.A.	Investigative	[7]
dihydrocarveol	DMS4U68	Discovery agent	N.A.	Investigative	[3]
diphenylboronic anhydride	DMRQZTS	Discovery agent	N.A.	Investigative	[8]
diphenyltetrahydrofuran	DMK8T61	Discovery agent	N.A.	Investigative	[8]
EDP-18	DMTVRKG	Major depressive disorder	6A70.3	Investigative	[9]
incensole acetate	DMONMHK	Discovery agent	N.A.	Investigative	[10]
tetrahydrocannabivarin	DMDY1MZ	Discovery agent	N.A.	Investigative	[11]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Major depressive disorder	6A20	Pre-frontal cortex	7.58E-01	5.28E-03	0.05

References

• [1] Pharmacological profiling of the TRPV3 channel in recombinant and native assays. Br J Pharmacol. 2014 May;171(10):2631-44.
• [2] 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3. J Neurosci. 2004 Jun 2;24(22):5177-82.
• [3] Monoterpenoid agonists of TRPV3. Br J Pharmacol. 2007 Jun;151(4):530-40.
• [4] 17(R)-resolvin D1 specifically inhibits transient receptor potential ion channel vanilloid 3 leading to peripheral antinociception. Br J Pharmacol. 2012 Feb;165(3):683-92.
• [5] Oregano, thyme and clove-derived flavors and skin sensitizers activate specific TRP channels. Nat Neurosci. 2006 May;9(5):628-35.
• [6] More than cool: promiscuous relationships of menthol and other sensory compounds. Mol Cell Neurosci. 2006 Aug;32(4):335-43.
• [7] Citral sensing by Transient [corrected] receptor potential channels in dorsal root ganglion neurons. PLoS One. 2008 May 7;3(5):e2082.
• [8] Biphasic currents evoked by chemical or thermal activation of the heat-gated ion channel, TRPV3. J Biol Chem. 2005 Apr 22;280(16):15928-41.
• [9] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 509).
• [10] Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. FASEB J. 2008 Aug;22(8):3024-34.
• [11] Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. Acta Physiol (Oxf). 2012 Feb;204(2):255-66.