Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJW7B3)

• DTT Name: P2X purinoceptor 1 (P2RX1)
• Synonyms: Purinergic receptor 1; P2X1
• Gene Name: P2RX1
• DTT Type: Literature-reported target; [1]
• UniProt ID: P2RX1_HUMAN
• TTD ID: T69091
• Sequence:
  MARRFQEELAAFLFEYDTPRMVLVRNKKVGVIFRLIQLVVLVYVIGWVFLYEKGYQTSSG
  LISSVSVKLKGLAVTQLPGLGPQVWDVADYVFPAQGDNSFVVMTNFIVTPKQTQGYCAEH
  PEGGICKEDSGCTPGKAKRKAQGIRTGKCVAFNDTVKTCEIFGWCPVEVDDDIPRPALLR
  EAENFTLFIKNSISFPRFKVNRRNLVEEVNAAHMKTCLFHKTLHPLCPVFQLGYVVQESG
  QNFSTLAEKGGVVGITIDWHCDLDWHVRHCRPIYEFHGLYEEKNLSPGFNFRFARHFVEN
  GTNYRHLFKVFGIRFDILVDGKAGKFDIIPTMTTIGSGIGIFGVATVLCDLLLLHILPKR
  HYYKQKKFKYAEDMGPGAAERDLAATSSTLGLQENMRTS
• Function: Ligand-gated ion channel with relatively high calcium permeability. Binding to ATP mediates synaptic transmission between neurons and from neurons to smooth muscle. Seems to be linked to apoptosis, by increasing the intracellular concentration of calcium in the presence of ATP, leading to programmed cell death (By similarity).
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Platelet activation (hsa04611)
• Reactome Pathway:
  Platelet homeostasis (R-HSA-418346)
  Neutrophil degranulation (R-HSA-6798695)
  Elevation of cytosolic Ca2+ levels (R-HSA-139853)

Molecular Interaction Atlas (MIA) of This DTT

7 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BzATP	DM37GYA	Discovery agent	N.A.	Investigative	[2]
Ip5I	DMB2YXN	Discovery agent	N.A.	Investigative	[2]
L-betagamma-meATP	DMTNQCE	Discovery agent	N.A.	Investigative	[2]
MRS 2219	DM7IK68	Discovery agent	N.A.	Investigative	[1]
NF023	DMJ4GO9	Discovery agent	N.A.	Investigative	[2]
NF449	DM816Z2	Discovery agent	N.A.	Investigative	[3]
TNP-ATP	DMVZY0X	Discovery agent	N.A.	Investigative	[4]

References

• [1] A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. J Med Chem. 1998 Jun 18;41(13):2201-6.
• [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: 478).
• [3] Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. Eur J Med Chem. 2004 Apr;39(4):345-57.
• [4] Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. Mol Pharmacol. 1998 Jun;53(6):969-73.