Details of the Target

General Information of Target

Target ID LDTP13774
Target Name Short transient receptor potential channel 6 (TRPC6)
Gene Name TRPC6
Gene ID 7225
Synonyms
TRP6; Short transient receptor potential channel 6; TrpC6; Transient receptor protein 6; TRP-6
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
NKSKKRRNRVSFLGAATVEPPKPIPLTWKTEKPVWVNQWPLPKQKLEALHLLANEQLEKG
HIEPSFSPWNSPVFVIQKKSGKWRMLTDLRAVNAVNAVIQPMGPLQPGLPSLAMIPKDWP
LIIIDLKDCFFTIPLAEQDCEKFAFTIPAINNKEPATRFQWKVLPQGMLNSPTICQTFVG
RALQPVREKFSDCYIIHYIDDILCAAEMKDKLIDCYTFLQAEVANAGLAIASDKIQTSTP
FHYLEMQIENRKIKPPKIEIRKDTLKTLNDFQKLLGDINWIRPTLGIPTYAMSNLFSILR
GDSDLNSKRMLTPEATKEIKLVEEKIQSAQINRIDPLAPLQLLIFATAHSPTGIIIQNTD
LVEWSFLPHSTVKTFTLYLDQMATLIGQTRLRIIKLCGNDPDKIVVPLTKEQVRQAFINS
GAWQIGLANFVGIIDNHYPKTKIFQFLKMTTWILPKITRREPLENALTVFTDGSSNGKAA
YTGPKERVIKTQYQSAQRAELVAVITVLQDFDQPINIISDSAYVVQATRDVETALIKYSM
DDQLNQLFNLLQQTVRKRNFPFYITHIRAHTNLPGPLTKANEQADLLVSSALIKAQELHA
LTHVNVAGLKNKFDVTWKQAKDIVQHCTQCQVLHLPTQEAGVNPRGLCPNALWQMDVTHV
SSFGRLSYIHVTVDTYSHFIWATCQTGESTSHVKKHLLSCFAVMGVPEKIKTDNGPGYCS
KAFQKFLSQWKISHTTGIPYNSQGQAIVERTNRTLKTQLVKQKEGGDSKECTTPQMQLNL
ALYTLNFLNIYRNQTTTSAEQHLTGKKNSPHEGKLIWWKDNKNKTWEIGKVITWGRGFAC
VSPGENQLPVWIPTRHLKFYNEPIGDAKKSTSAETETPQSSTVDSQDEQNGDVRRTDEVA
IHQESRAADLGTTKEADAVSYKISREHKGDTNPREYAACGLDDCINGGKSPYACRSSCS
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Transient receptor (TC 1.A.4) family, STrpC subfamily, TRPC6 sub-subfamily
Subcellular location
Cell membrane
Function
Thought to form a receptor-activated non-selective calcium permeant cation channel. Probably is operated by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases or G-protein coupled receptors. Activated by diacylglycerol (DAG) in a membrane-delimited fashion, independently of protein kinase C. Seems not to be activated by intracellular calcium store depletion.
TTD ID
T80165
Uniprot ID
Q9Y210
DrugMap ID
TTRBT3W
Ensemble ID
ENST00000344327.8
HGNC ID
HGNC:12338
ChEMBL ID
CHEMBL2417347

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.R25H .
DU145 SNV: p.S170T; p.S836N .
G361 SNV: p.D736N .
HCC1954 SNV: p.W526C .
HLF SNV: p.A535S .
HS936T SNV: p.E881K .
HT115 SNV: p.E313A .
MDAMB453 SNV: p.P361Q .
NCIH2172 SNV: p.Q624H .
NCIH23 SNV: p.L398S .
NCIH661 SNV: p.K781R .
SAOS2 SNV: p.N694H .
SHSY5Y SNV: p.G109C .
SNU1 Deletion: p.G794VfsTer8 .
SW1271 SNV: p.A543S .
SW480 SNV: p.I223N .
TF1 SNV: p.D35Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C267(1.00)  LDD3314  [1]
IA-alkyne
 Probe Info  		2.33  LDD2183  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0576  Fragment14 Ramos 1.12  LDD2193  [2]
 LDCM0566  Fragment4 Ramos 0.56  LDD2184  [2]
 LDCM0569  Fragment7 Ramos 0.60  LDD2186  [2]
 LDCM0022  KB02 CAL-51 C267(1.00)  LDD2288  [1]
 LDCM0023  KB03 Ramos 2.33  LDD2183  [2]
 LDCM0024  KB05 IGR37 C267(1.00)  LDD3314  [1]

References

1 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
2 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578