Target Information
Target General Infomation | |||||
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Target ID |
T49526
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Former ID |
TTDS00148
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Target Name |
Potassium voltage-gated channel subfamily KQT member 1
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Gene Name |
KCNQ1
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Synonyms |
IKs producing slow voltage-gated potassium channel alpha subunit KvLQT1; KCNQ1 channel; KQT-like 1; Kv7.1; Voltage-gated potassium channel subunit Kv7.1; KCNQ1
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Target Type |
Successful
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Disease | Hypertension [ICD9: 401; ICD10: I10-I16] | ||||
Function |
Probably important in cardiac repolarization. associates with kcne1 (mink) to form the i(ks) cardiac potassium current. elicits a rapidly activating, potassium-selective outward current. Muscarinic agonist oxotremorinem strongly suppresses kcnq1/kcne1.
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BioChemical Class |
Voltage-gated ion channel
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Target Validation |
T49526
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UniProt ID | |||||
Sequence |
MAAASSPPRAERKRWGWGRLPGARRGSAGLAKKCPFSLELAEGGPAGGALYAPIAPGAPG
PAPPASPAAPAAPPVASDLGPRPPVSLDPRVSIYSTRRPVLARTHVQGRVYNFLERPTGW KCFVYHFAVFLIVLVCLIFSVLSTIEQYAALATGTLFWMEIVLVVFFGTEYVVRLWSAGC RSKYVGLWGRLRFARKPISIIDLIVVVASMVVLCVGSKGQVFATSAIRGIRFLQILRMLH VDRQGGTWRLLGSVVFIHRQELITTLYIGFLGLIFSSYFVYLAEKDAVNESGRVEFGSYA DALWWGVVTVTTIGYGDKVPQTWVGKTIASCFSVFAISFFALPAGILGSGFALKVQQKQR QKHFNRQIPAAASLIQTAWRCYAAENPDSSTWKIYIRKAPRSHTLLSPSPKPKKSVVVKK KKFKLDKDNGVTPGEKMLTVPHITCDPPEERRLDHFSVDGYDSSVRKSPTLLEVSMPHFM RTNSFAEDLDLEGETLLTPITHISQLREHHRATIKVIRRMQYFVAKKKFQQARKPYDVRD VIEQYSQGHLNLMVRIKELQRRLDQSIGKPSLFISVSEKSKDRGSNTIGARLNRVEDKVT QLDQRLALITDMLHQLLSLHGGSTPGSGGPPREGGAHITQPCGSGGSVDPELFLPSNTLP TYEQLTVPRRGPDEGS |
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Drugs and Mode of Action | |||||
Blocker (channel blocker) | (3R,4S)-293B | Drug Info | [526219] | ||
3S,4R-293B | Drug Info | [526219] | |||
IKs124 | Drug Info | [527319] | |||
XE991 | Drug Info | [525778] | |||
Inhibitor | HMR-1556 | Drug Info | [526979] | ||
L-768673 | Drug Info | [534526] | |||
N-(2-Diethylamino-ethyl)-4-hexyloxy-benzamide | Drug Info | [526184] | |||
N-(3,3-Dimethyl-butyl)-4-hexyloxy-benzamide | Drug Info | [526184] | |||
N-(3,3-Dimethyl-butyl)-4-indol-1-yl-benzamide | Drug Info | [526184] | |||
N-(3,3-Dimethyl-cyclopentyl)-4-hexyloxy-benzamide | Drug Info | [526184] | |||
Blocker | Indapamide | Drug Info | [536209] | ||
L-735,821 | Drug Info | [535746] | |||
Activator | ML277 | Drug Info | [532012] | ||
R-L3 | Drug Info | [534668] | |||
zinc pyrithione | Drug Info | [528790] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Adrenergic signaling in cardiomyocytes | ||||
Cholinergic synapse | |||||
Gastric acid secretion | |||||
Pancreatic secretion | |||||
Protein digestion and absorption | |||||
Vibrio cholerae infection | |||||
PathWhiz Pathway | Muscle/Heart Contraction | ||||
Reactome | Voltage gated Potassium channels | ||||
WikiPathways | SIDS Susceptibility Pathways | ||||
Potassium Channels | |||||
miR-targeted genes in muscle cell - TarBase | |||||
miR-targeted genes in lymphocytes - TarBase | |||||
TarBasePathway | |||||
References | |||||
Ref 538270 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074299. | ||||
Ref 525778 | Molecular basis for differential sensitivity of KCNQ and I(Ks) channels to the cognitive enhancer XE991. Mol Pharmacol. 2000 Jun;57(6):1218-23. | ||||
Ref 526184 | J Med Chem. 2001 Nov 8;44(23):3764-7.Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers. | ||||
Ref 526219 | A kinetic study on the stereospecific inhibition of KCNQ1 and I(Ks) by the chromanol 293B. Br J Pharmacol. 2001 Dec;134(8):1647-54. | ||||
Ref 526979 | J Med Chem. 2004 Mar 11;47(6):1303-14.Selective optimization of side activities: another way for drug discovery. | ||||
Ref 527319 | Heteromeric KCNE2/KCNQ1 potassium channels in the luminal membrane of gastric parietal cells. J Physiol. 2004 Dec 1;561(Pt 2):547-57. Epub 2004 Oct 7. | ||||
Ref 528790 | Zinc 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 532012 | Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41. | ||||
Ref 534526 | J Med Chem. 1997 Nov 21;40(24):3865-8.Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide. | ||||
Ref 534668 | A novel benzodiazepine that activates cardiac slow delayed rectifier K+ currents. Mol Pharmacol. 1998 Jul;54(1):220-30. |
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