Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT329V4)

• DTT Name: Inward rectifier potassium channel Kir6.2 (KCNJ11)
• Synonyms: Potassium channel, inwardly rectifying, subfamily J, member 11; KCNJ11; KATP channel (Kir6.2/SUR2A); Inward rectifier K+ channel Kir6.2; IKATP
• Gene Name: KCNJ11
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Inward rectifier potassium channel
• UniProt ID: KCJ11_HUMAN
• TTD ID: T00820
• Sequence:
  MLSRKGIIPEEYVLTRLAEDPAEPRYRARQRRARFVSKKGNCNVAHKNIREQGRFLQDVF
  TTLVDLKWPHTLLIFTMSFLCSWLLFAMAWWLIAFAHGDLAPSEGTAEPCVTSIHSFSSA
  FLFSIEVQVTIGFGGRMVTEECPLAILILIVQNIVGLMINAIMLGCIFMKTAQAHRRAET
  LIFSKHAVIALRHGRLCFMLRVGDLRKSMIISATIHMQVVRKTTSPEGEVVPLHQVDIPM
  ENGVGGNSIFLVAPLIIYHVIDANSPLYDLAPSDLHHHQDLEIIVILEGVVETTGITTQA
  RTSYLADEILWGQRFVPIVAEEDGRYSVDYSKFGNTIKVPTPLCTARQLDEDHSLLEALT
  LASARGPLRKRSVPMAKAKPKFSISPDSLS
• Function: This receptor is controlled by G proteins. 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. Subunit of ATP-sensitive potassium channels (KATP). Can form cardiac and smooth muscle-type KATP channels with ABCC9. KCNJ11 forms the channel pore while ABCC9 is required for activation and regulation.
• KEGG Pathway:
  Insulin secretion (hsa04911)
  Type II diabetes mellitus (hsa04930)
• Reactome Pathway:
  Regulation of insulin secretion (R-HSA-422356)
  ABC-family proteins mediated transport (R-HSA-382556)

Molecular Interaction Atlas (MIA) of This DTT

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HBR-985	DMKDBFL	Discovery agent	N.A.	Investigative	[1]

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: ATP-sensitive inward rectifier potassium channel 11 (KCNJ11) DTP Info
• Gene Name: KCNJ11

References

• [1] Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98.