Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT9R6BE)

• DTT Name: Calcium-activated potassium channel KCa2.1 (KCNN1)
• Synonyms: Small conductance calcium-activated potassium channel protein 1; SKCa1; SKCa 1; SK1; SK; KCa2.1
• Gene Name: KCNN1
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Voltage-gated ion channel
• UniProt ID: KCNN1_HUMAN
• TTD ID: T11911
• Sequence:
  MNSHSYNGSVGRPLGSGPGALGRDPPDPEAGHPPQPPHSPGLQVVVAKSEPARPSPGSPR
  GQPQDQDDDEDDEEDEAGRQRASGKPSNVGHRLGHRRALFEKRKRLSDYALIFGMFGIVV
  MVTETELSWGVYTKESLYSFALKCLISLSTAILLGLVVLYHAREIQLFMVDNGADDWRIA
  MTCERVFLISLELAVCAIHPVPGHYRFTWTARLAFTYAPSVAEADVDVLLSIPMFLRLYL
  LGRVMLLHSKIFTDASSRSIGALNKITFNTRFVMKTLMTICPGTVLLVFSISSWIIAAWT
  VRVCERYHDKQEVTSNFLGAMWLISITFLSIGYGDMVPHTYCGKGVCLLTGIMGAGCTAL
  VVAVVARKLELTKAEKHVHNFMMDTQLTKRVKNAAANVLRETWLIYKHTRLVKKPDQARV
  RKHQRKFLQAIHQAQKLRSVKIEQGKLNDQANTLTDLAKTQTVMYDLVSELHAQHEELEA
  RLATLESRLDALGASLQALPGLIAQAIRPPPPPLPPRPGPGPQDQAARSSPCRWTPVAPS
  DCG
• Function: Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin (By similarity).
• KEGG Pathway:
  Insulin secretion (hsa04911)
  GnRH secretion (hsa04929)
• Reactome Pathway: Ca2+ activated K+ channels (R-HSA-1296052)

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
dequalinium	DMXM19W	Myelopathy	8B42	Clinical trial	[1]

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
apamin	DMYNBK5	Discovery agent	N.A.	Investigative	[1]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[2]
UCL1684	DMZNJFU	Discovery agent	N.A.	Investigative	[2]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[3]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[2]

The Drug Transporter (DTP) Role of This DTT

• DTT DTP Name: Small conductance calcium-activated potassium channel protein 1 (KCNN1) DTP Info
• Gene Name: KCNN1

References

• [1] Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells. Br J Pharmacol. 2000 Mar;129(5):991-9.
• [2] Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55.
• [3] The pharmacology of hSK1 Ca2+-activated K+ channels expressed in mammalian cell lines. Br J Pharmacol. 2000 Feb;129(4):627-30.