Target Information

Target General Infomation
Target ID
T74483
Former ID
TTDR00544
Target Name
Potassium voltage-gated channel subfamily KQT member 2
Gene Name
KCNQ2
Synonyms
K+ channel KCNQ2; KQT-like 2; Neuroblastoma-specific potassium channel KQT-like 2; Neuroblastoma-specific potassium channel alpha subunit KvLQT2; Voltage-gated potassium channel subunit Kv7.2; KCNQ2
Target Type
Research
Disease Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Probably importantin the regulation of neuronal excitability. Associates with kcnq3 to form a potassium channel with essentially identical properties to the channel underlying the native m-current.
BioChemical Class
Voltage-gated ion channel
UniProt ID
O43526
Sequence
MVQKSRNGGVYPGPSGEKKLKVGFVGLDPGAPDSTRDGALLIAGSEAPKRGSILSKPRAG
GAGAGKPPKRNAFYRKLQNFLYNVLERPRGWAFIYHAYVFLLVFSCLVLSVFSTIKEYEK
SSEGALYILEIVTIVVFGVEYFVRIWAAGCCCRYRGWRGRLKFARKPFCVIDIMVLIASI
AVLAAGSQGNVFATSALRSLRFLQILRMIRMDRRGGTWKLLGSVVYAHSKELVTAWYIGF
LCLILASFLVYLAEKGENDHFDTYADALWWGLITLTTIGYGDKYPQTWNGRLLAATFTLI
GVSFFALPAGILGSGFALKVQEQHRQKHFEKRRNPAAGLIQSAWRFYATNLSRTDLHSTW
QYYERTVTVPMYSSQTQTYGASRLIPPLNQLELLRNLKSKSGLAFRKDPPPEPSPSKGSP
CRGPLCGCCPGRSSQKVSLKDRVFSSPRGVAAKGKGSPQAQTVRRSPSADQSLEDSPSKV
PKSWSFGDRSRARQAFRIKGAASRQNSEEASLPGEDIVDDKSCPCEFVTEDLTPGLKVSI
RAVCVMRFLVSKRKFKESLRPYDVMDVIEQYSAGHLDMLSRIKSLQSRVDQIVGRGPAIT
DKDRTKGPAEAELPEDPSMMGRLGKVEKQVLSMEKKLDFLVNIYMQRMGIPPTETEAYFG
AKEPEPAPPYHSPEDSREHVDRHGCIVKIVRSSSSTGQKNFSAPPAAPPVQCPPSTSWQP
QSHPRQGHGTSPVGDHGSLVRIPPPPAHERSLSAYGGGNRASMEFLRQEDTPGCRPPEGN
LRDSDTSISIPSVDHEELERSFSGFSISQSKENLDALNSCYAAVAPCAKVRPYIAEGESD
TDSDLCTPCGPPPRSATGEGPFGDVGWAGPRK
Drugs and Mode of Action
Drug(s) ICA-69673 Drug Info Preclinical Pain [546904]
Activator (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide Drug Info [528363]
ICA-27243 Drug Info [530361]
PIP2 Drug Info [527827]
QO-58 Drug Info [532057]
zinc pyrithione Drug Info [528790]
ztz240 Drug Info [530996]
Modulator ICA-69673 Drug Info
Inhibitor PD-32577 Drug Info [525576]
Blocker (channel blocker) tetraethylammonium Drug Info [525854]
XE991 Drug Info [534766]
Pathways
KEGG Pathway Cholinergic synapse
PANTHER Pathway Muscarinic acetylcholine receptor 1 and 3 signaling pathway
Reactome Voltage gated Potassium channels
Interaction between L1 and Ankyrins
WikiPathways Potassium Channels
L1CAM interactions
References
Ref 546904Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011004)
Ref 525576Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Ref 525854Mol Pharmacol. 2000 Sep;58(3):591-600.Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.
Ref 527827Regulation of Kv7 (KCNQ) K+ channel open probability by phosphatidylinositol 4,5-bisphosphate. J Neurosci. 2005 Oct 26;25(43):9825-35.
Ref 528363The acrylamide (S)-1 differentially affects Kv7 (KCNQ) potassium channels. Neuropharmacology. 2006 Nov;51(6):1068-77. Epub 2006 Aug 10.
Ref 528790Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants. Nat Chem Biol. 2007 May;3(5):287-96. Epub 2007 Apr 15.
Ref 530361The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site. Neurosci Lett. 2009 Nov 13;465(2):138-42.
Ref 530996Isoform-specific prolongation of Kv7 (KCNQ) potassium channel opening mediated by new molecular determinants for drug-channel interactions. J Biol Chem. 2010 Sep 3;285(36):28322-32.
Ref 532057Modulation of K(v)7 potassium channels by a novel opener pyrazolo[1,5-a]pyrimidin-7(4H)-one compound QO-58. Br J Pharmacol. 2013 Feb;168(4):1030-42.
Ref 534766KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998 Dec 4;282(5395):1890-3.

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