Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTH7UO3)

• DTT Name: Inward rectifier potassium channel Kir2.1 (KCNJ2)
• Synonyms: hIRK1; Potassium channel, inwardly rectifying subfamily J member 2; Inward rectifier K(+) channel Kir2.1; IRK1; IRK-1; Cardiac inward rectifier potassium channel
• Gene Name: KCNJ2
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Inward rectifier potassium channel
• UniProt ID: KCNJ2_HUMAN
• TTD ID: T74570
• Sequence:
  MGSVRTNRYSIVSSEEDGMKLATMAVANGFGNGKSKVHTRQQCRSRFVKKDGHCNVQFIN
  VGEKGQRYLADIFTTCVDIRWRWMLVIFCLAFVLSWLFFGCVFWLIALLHGDLDASKEGK
  ACVSEVNSFTAAFLFSIETQTTIGYGFRCVTDECPIAVFMVVFQSIVGCIIDAFIIGAVM
  AKMAKPKKRNETLVFSHNAVIAMRDGKLCLMWRVGNLRKSHLVEAHVRAQLLKSRITSEG
  EYIPLDQIDINVGFDSGIDRIFLVSPITIVHEIDEDSPLYDLSKQDIDNADFEIVVILEG
  MVEATAMTTQCRSSYLANEILWGHRYEPVLFEEKHYYKVDYSRFHKTYEVPNTPLCSARD
  LAEKKYILSNANSFCYENEVALTSKEEDDSENGVPESTSTDTPPDIDLHNQASVPLEPRP
  LRRESEI
• Function: Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. Can be blocked by extracellular barium or cesium. Probably participates in establishing action potential waveform and excitability of neuronal and muscle tissues.
• KEGG Pathway:
  Cholinergic synapse (hsa04725)
  Oxytocin signaling pathway (hsa04921)
  Renin secretion (hsa04924)
  Gastric acid secretion (hsa04971)
• Reactome Pathway:
  Classical Kir channels (R-HSA-1296053)
  Phase 4 - resting membrane potential (R-HSA-5576886)
  Sensory perception of sour taste (R-HSA-9729555)
  Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits (R-HSA-997272)
  Activation of G protein gated Potassium channels (R-HSA-1296041)

Molecular Interaction Atlas (MIA) of This DTT

2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
oleoyl-CoA	DMJ1VRU	Discovery agent	N.A.	Investigative	[1]
PIP2	DMOZV7N	Discovery agent	N.A.	Investigative	[2]

References

• [1] Cytoplasmic accumulation of long-chain coenzyme A esters activates KATP and inhibits Kir2.1 channels. J Physiol. 2006 Sep 1;575(Pt 2):433-42.
• [2] Multiple PIP2 binding sites in Kir2.1 inwardly rectifying potassium channels. FEBS Lett. 2001 Feb 9;490(1-2):49-53.