Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTRBT3W)

• DTT Name: Short transient receptor potential channel 6 (TRPC6)
• Synonyms: TRPC6; TRP6; STrpC6
• Gene Name: TRPC6
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Transient receptor potential catioin channel
• UniProt ID: TRPC6_HUMAN
• TTD ID: T80165
• Sequence:
  MSQSPAFGPRRGSSPRGAAGAAARRNESQDYLLMDSELGEDGCPQAPLPCYGYYPCFRGS
  DNRLAHRRQTVLREKGRRLANRGPAYMFSDRSTSLSIEEERFLDAAEYGNIPVVRKMLEE
  CHSLNVNCVDYMGQNALQLAVANEHLEITELLLKKENLSRVGDALLLAISKGYVRIVEAI
  LSHPAFAEGKRLATSPSQSELQQDDFYAYDEDGTRFSHDVTPIILAAHCQEYEIVHTLLR
  KGARIERPHDYFCKCNDCNQKQKHDSFSHSRSRINAYKGLASPAYLSLSSEDPVMTALEL
  SNELAVLANIEKEFKNDYKKLSMQCKDFVVGLLDLCRNTEEVEAILNGDVETLQSGDHGR
  PNLSRLKLAIKYEVKKFVAHPNCQQQLLSIWYENLSGLRQQTMAVKFLVVLAVAIGLPFL
  ALIYWFAPCSKMGKIMRGPFMKFVAHAASFTIFLGLLVMNAADRFEGTKLLPNETSTDNA
  KQLFRMKTSCFSWMEMLIISWVIGMIWAECKEIWTQGPKEYLFELWNMLDFGMLAIFAAS
  FIARFMAFWHASKAQSIIDANDTLKDLTKVTLGDNVKYYNLARIKWDPSDPQIISEGLYA
  IAVVLSFSRIAYILPANESFGPLQISLGRTVKDIFKFMVIFIMVFVAFMIGMFNLYSYYI
  GAKQNEAFTTVEESFKTLFWAIFGLSEVKSVVINYNHKFIENIGYVLYGVYNVTMVIVLL
  NMLIAMINSSFQEIEDDADVEWKFARAKLWFSYFEEGRTLPVPFNLVPSPKSLFYLLLKL
  KKWISELFQGHKKGFQEDAEMNKINEEKKLGILGSHEDLSKLSLDKKQVGHNKQPSIRSS
  EDFHLNSFNNPPRQYQKIMKRLIKRYVLQAQIDKESDEVNEGELKEIKQDISSLRYELLE
  EKSQNTEDLAELIRELGEKLSMEPNQEETNR
• 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.
• KEGG Pathway:
  cGMP-PKG signaling pathway (hsa04022)
  Axon guidance (hsa04360)
• Reactome Pathway:
  TRP channels (R-HSA-3295583)
  Role of second messengers in netrin-1 signaling (R-HSA-418890)
  Effects of PIP2 hydrolysis (R-HSA-114508)

Molecular Interaction Atlas (MIA) of This DTT

11 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]
20-HETE	DM5BAJ9	Discovery agent	N.A.	Investigative	[2]
ACAA	DMACYPW	Discovery agent	N.A.	Investigative	[2]
flufenamate	DMN8AP0	Discovery agent	N.A.	Investigative	[2]
hyp 9	DM0U8IV	Discovery agent	N.A.	Investigative	[3]
KB-R7943	DMMD5W3	Discovery agent	N.A.	Investigative	[2]
lysophosphatidylcholine	DMOGFVH	Discovery agent	N.A.	Investigative	[2]
ML9	DMP13VE	Discovery agent	N.A.	Investigative	[2]
OAG	DMOP8IJ	Discovery agent	N.A.	Investigative	[1]
SAG	DMHOG7W	Discovery agent	N.A.	Investigative	[1]
SLG	DMEBPCO	Discovery agent	N.A.	Investigative	[1]

References

• [1] Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol. Nature. 1999 Jan 21;397(6716):259-63.
• [2] 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: 491).
• [3] Simple 2,4-diacylphloroglucinols as classic transient receptor potential-6 activators--identification of a novel pharmacophore. Mol Pharmacol. 2010 Mar;77(3):368-77.