Details of the Target

General Information of Target

Target ID LDTP14154
Target Name Transient receptor potential cation channel subfamily V member 2 (TRPV2)
Gene Name TRPV2
Gene ID 51393
Synonyms
VRL; Transient receptor potential cation channel subfamily V member 2; TrpV2; Osm-9-like TRP channel 2; OTRPC2; Vanilloid receptor-like protein 1; VRL-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTVHNLYLFDRNGVCLHYSEWHRKKQAGIPKEEEYKLMYGMLFSIRSFVSKMSPLDMKDG
FLAFQTSRYKLHYYETPTGIKVVMNTDLGVGPIRDVLHHIYSALYVELVVKNPLCPLGQT
VQSELFRSRLDSYVRSLPFFSARAG
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Transient receptor (TC 1.A.4) family, TrpV subfamily, TRPV2 sub-subfamily
Subcellular location
Cell membrane
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.
TTD ID
T82267
Uniprot ID
Q9Y5S1
DrugMap ID
TTBECWA
Ensemble ID
ENST00000338560.12
HGNC ID
HGNC:18082
ChEMBL ID
CHEMBL5051

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		8.66  LDD0402  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
DBIA
 Probe Info  		C332(1.89)  LDD3325  [3]
AHL-Pu-1
 Probe Info  		C156(2.55)  LDD0170  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C156(2.55)  LDD0170  [4]
 LDCM0026  4SU-RNA+native RNA DM93 C722(2.01); C349(2.40)  LDD0171  [4]
 LDCM0022  KB02 22RV1 C722(0.78)  LDD2243  [3]
 LDCM0023  KB03 22RV1 C722(0.82)  LDD2660  [3]
 LDCM0024  KB05 UACC257 C332(1.89)  LDD3325  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cannabidiol Small molecular drug DB09061
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-apb Small molecular drug D00HCI
Cannabinol Small molecular drug D0U5LL
Citral Small molecular drug D00VWN
Diphenylboronic Anhydride Small molecular drug D03TWR
Lysophosphatidylcholine Small molecular drug D0KT5E
Lysophosphatidylinositol Small molecular drug D0M1UA
Nabiximols Small molecular drug DB14011
Tetrahydrocannabivarin Small molecular drug DB11755
Trim Small molecular drug D0B3AR
[14c]Tea Small molecular drug D06PZZ
Cannabidivarin . DB14050
Medical Cannabis . DB14009

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
4 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625