Target Information
Target General Infomation | |||||
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Target ID |
T76914
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Former ID |
TTDR00903
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Target Name |
Potassium voltage-gated channel subfamily A member 3
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Gene Name |
KCNA3
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Synonyms |
HGK5; HLK3; HPCN3; HuKIII; Potassium channel Kv1.3; Voltage-gated K(+) channel Kv1.3; Voltage-gated Kv1.3 K(+) channel; Voltage-gated potassium channel subunit Kv1.3; KCNA3
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Target Type |
Clinical Trial
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Disease | Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | ||||
Psoriatic arthritis [ICD9: 696; ICD10: L40.5, M07] | |||||
Function |
Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel through which potassium ions may pass in accordance with their electrochemical gradient.
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BioChemical Class |
Voltage-gated ion channel
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Target Validation |
T76914
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UniProt ID | |||||
Sequence |
MDERLSLLRSPPPPSARHRAHPPQRPASSGGAHTLVNHGYAEPAAGRELPPDMTVVPGDH
LLEPEVADGGGAPPQGGCGGGGCDRYEPLPPSLPAAGEQDCCGERVVINISGLRFETQLK TLCQFPETLLGDPKRRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRIRRPVNVPIDIF SEEIRFYQLGEEAMEKFREDEGFLREEERPLPRRDFQRQVWLLFEYPESSGPARGIAIVS VLVILISIVIFCLETLPEFRDEKDYPASTSQDSFEAAGNSTSGSRAGASSFSDPFFVVET LCIIWFSFELLVRFFACPSKATFSRNIMNLIDIVAIIPYFITLGTELAERQGNGQQAMSL AILRVIRLVRVFRIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAE ADDPTSGFSSIPDAFWWAVVTMTTVGYGDMHPVTIGGKIVGSLCAIAGVLTIALPVPVIV SNFNYFYHRETEGEEQSQYMHVGSCQHLSSSAEELRKARSNSTLSKSEYMVIEEGGMNHS AFPQTPFKTGNSTATCTTNNNPNSCVNIKKIFTDV |
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Drugs and Mode of Action | |||||
Inhibitor | 1-Benzyl-7-chloro-4-hexyloxy-quinolinium | Drug Info | [533627] | ||
2-Methoxy-N-(3-methyl-2-phenyl-butyl)-benzamide | Drug Info | [526574] | |||
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one | Drug Info | [531235] | |||
5-(4-Phenylbutoxy)psoralen | Drug Info | [531233] | |||
Correloid | Drug Info | [527342] | |||
Correloid derivative | Drug Info | [527342] | |||
CP-339818 | Drug Info | [526035] | |||
Debio-0824 | Drug Info | [544248] | |||
UK-78282 | Drug Info | [526035] | |||
[1-Benzyl-1H-quinolin-(4E)-ylidene]-hexyl-amine | Drug Info | [533627] | |||
Blocker (channel blocker) | 5-(4-phenoxybutoxy)psoralen | Drug Info | [527687] | ||
correolide | Drug Info | [525474] | |||
tetraethylammonium | Drug Info | [533612] | |||
Blocker | Psora-4 | Drug Info | [535968] | ||
Pathways | |||||
References | |||||
Ref 525474 | Identification and biochemical characterization of a novel nortriterpene inhibitor of the human lymphocyte voltage-gated potassium channel, Kv1.3. Biochemistry. 1999 Apr 20;38(16):4922-30. | ||||
Ref 526035 | J Med Chem. 2001 Apr 12;44(8):1249-56.Angular methoxy-substituted furo- and pyranoquinolinones as blockers of the voltage-gated potassium channel Kv1.3. | ||||
Ref 526574 | Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4.Benzamide derivatives as blockers of Kv1.3 ion channel. | ||||
Ref 527342 | Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51.Potent Kv1.3 inhibitors from correolide-modification of the C18 position. | ||||
Ref 527687 | Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases. Mol Pharmacol. 2005 Nov;68(5):1254-70. Epub 2005 Aug 11. | ||||
Ref 531233 | Bioorg Med Chem Lett. 2010 Dec 1;20(23):6983-8. Epub 2010 Oct 7.N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1. | ||||
Ref 531235 | Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92. Epub 2010 Oct 23.Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. | ||||
Ref 533612 | Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. Mol Pharmacol. 1994 Jun;45(6):1227-34. | ||||
Ref 533627 | J Med Chem. 1995 May 26;38(11):1877-83.Novel inhibitors of potassium ion channels on human T lymphocytes. |
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