Target General Infomation
Target ID
T86271
Former ID
TTDI03308
Target Name
KCa2.2
Gene Name
KCNN2
Synonyms
KCNN2
Target Type
Clinical Trial
Disease Myeloneuropathy [ICD10: G04.1]
Myeloma disease [ICD9: 203; ICD10: C90]
UniProt ID
Sequence
MSSCRYNGGVMRPLSNLSASRRNLHEMDSEAQPLQPPASVGGGGGASSPSAAAAAAAAVS
SSAPEIVVSKPEHNNSNNLALYGTGGGGSTGGGGGGGGSGHGSSSGTKSSKKKNQNIGYK
LGHRRALFEKRKRLSDYALIFGMFGIVVMVIETELSWGAYDKASLYSLALKCLISLSTII
LLGLIIVYHAREIQLFMVDNGADDWRIAMTYERIFFICLEILVCAIHPIPGNYTFTWTAR
LAFSYAPSTTTADVDIILSIPMFLRLYLIARVMLLHSKLFTDASSRSIGALNKINFNTRF
VMKTLMTICPGTVLLVFSISLWIIAAWTVRACERYHDQQDVTSNFLGAMWLISITFLSIG
YGDMVPNTYCGKGVCLLTGIMGAGCTALVVAVVARKLELTKAEKHVHNFMMDTQLTKRVK
NAAANVLRETWLIYKNTKLVKKIDHAKVRKHQRKFLQAIHQLRSVKMEQRKLNDQANTLV
DLAKTQNIMYDMISDLNERSEDFEKRIVTLETKLETLIGSIHALPGLISQTIRQQQRDFI
EAQMESYDKHVTYNAERSRSSSRRRRSSSTAPPTSSESS
Drugs and Mode of Action
Drug(s) dequalinium Drug Info Clinical trial Myeloneuropathy [1]
zoxazolamine Drug Info Terminated Myeloma disease [2]
Blocker (channel blocker) apamin Drug Info [3]
dequalinium Drug Info [4]
tetraethylammonium Drug Info [5]
UCL1684 Drug Info [6]
UCL1848 Drug Info [7]
Activator CyPPA Drug Info [8]
DC-EBIO Drug Info [9]
EBIO Drug Info [5]
zoxazolamine Drug Info [10]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
REF 1Pharmacological characterisation of the human small conductance calcium-activated potassium channel hSK3 reveals sensitivity to tricyclic antidepressants and antipsychotic phenothiazines. Neuropharmacology. 2001 May;40(6):772-83.
REF 2(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. (Ligand id: 2327).
REF 3SK2 encodes the apamin-sensitive Ca(2+)-activated K(+) channels in the human leukemic T cell line, Jurkat. FEBS Lett. 2000 Mar 10;469(2-3):196-202.
REF 4Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds. Eur J Pharmacol. 2000 Jul 28;401(1):1-7.
REF 5Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55.
REF 6Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells. Br J Pharmacol. 2000 Mar;129(5):991-9.
REF 7Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels. J Biol Chem. 2001 Apr 13;276(15):12249-56. Epub 2001 Jan 22.
REF 8Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels. Br J Pharmacol. 2007 Jul;151(5):655-65. Epub 2007 May 8.
REF 9Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons. J Biol Chem. 2005 Dec16;280(50):41404-11. Epub 2005 Oct 20.
REF 10Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds. J Pharmacol Exp Ther. 2001 Mar;296(3):683-9.

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