Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Transient receptor potential cation channel V2 (TRPV2)
• Synonyms: Vanilloid receptor-like protein 1; VRL-1; VRL; TrpV2; Transient receptor potential cation channel subfamily V member 2; Osm-9-like TRP channel 2; OTRPC2
• Gene Name: TRPV2
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Transient receptor potential catioin channel
• UniProt ID: TRPV2_HUMAN
• TTD ID: T82267
• Sequence:
  MTSPSSSPVFRLETLDGGQEDGSEADRGKLDFGSGLPPMESQFQGEDRKFAPQIRVNLNY
  RKGTGASQPDPNRFDRDRLFNAVSRGVPEDLAGLPEYLSKTSKYLTDSEYTEGSTGKTCL
  MKAVLNLKDGVNACILPLLQIDRDSGNPQPLVNAQCTDDYYRGHSALHIAIEKRSLQCVK
  LLVENGANVHARACGRFFQKGQGTCFYFGELPLSLAACTKQWDVVSYLLENPHQPASLQA
  TDSQGNTVLHALVMISDNSAENIALVTSMYDGLLQAGARLCPTVQLEDIRNLQDLTPLKL
  AAKEGKIEIFRHILQREFSGLSHLSRKFTEWCYGPVRVSLYDLASVDSCEENSVLEIIAF
  HCKSPHRHRMVVLEPLNKLLQAKWDLLIPKFFLNFLCNLIYMFIFTAVAYHQPTLKKQAA
  PHLKAEVGNSMLLTGHILILLGGIYLLVGQLWYFWRRHVFIWISFIDSYFEILFLFQALL
  TVVSQVLCFLAIEWYLPLLVSALVLGWLNLLYYTRGFQHTGIYSVMIQKVILRDLLRFLL
  IYLVFLFGFAVALVSLSQEAWRPEAPTGPNATESVQPMEGQEDEGNGAQYRGILEASLEL
  FKFTIGMGELAFQEQLHFRGMVLLLLLAYVLLTYILLLNMLIALMSETVNSVATDSWSIW
  KLQKAISVLEMENGYWWCRKKQRAGVMLTVGTKPDGSPDERWCFRVEEVNWASWEQTLPT
  LCEDPSGAGVPRTLENPVLASPPKEDEDGASEENYVPVQLLQSN
• Function: Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by IGF-I, PDGF and neuropeptide head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH.
• KEGG Pathway:
  NOD-like receptor signaling pathway (hsa04621)
  Inflammatory mediator regulation of TRP channels (hsa04750)
• Reactome Pathway: TRP channels (R-HSA-3295583)

Molecular Interaction Atlas (MIA) of This DTT

8 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-APB	DM9AKVR	Discovery agent	N.A.	Investigative	[1]
cannabinol	DMM6A7P	Discovery agent	N.A.	Investigative	[2]
citral	DM53ZGY	Discovery agent	N.A.	Investigative	[3]
diphenylboronic anhydride	DMRQZTS	Discovery agent	N.A.	Investigative	[1]
lysophosphatidylcholine	DMOGFVH	Discovery agent	N.A.	Investigative	[4]
lysophosphatidylinositol	DMETM3R	Discovery agent	N.A.	Investigative	[4]
TRIM	DMNHU4M	Discovery agent	N.A.	Investigative	[1]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[1]

References

• [1] Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxy... Mol Pharmacol. 2007 Nov;72(5):1258-68.
• [2] TRPV2 is activated by cannabidiol and mediates CGRP release in cultured rat dorsal root ganglion neurons. J Neurosci. 2008 Jun 11;28(24):6231-8.
• [3] Citral sensing by Transient [corrected] receptor potential channels in dorsal root ganglion neurons. PLoS One. 2008 May 7;3(5):e2082.
• [4] Lysophospholipids stimulate prostate cancer cell migration via TRPV2 channel activation. Biochim Biophys Acta. 2009 Mar;1793(3):528-39.