Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| 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 | |||||
| Drug(s) | Debio-0824 | Drug Info | Phase 1 | Psoriatic arthritis | [1] |
| UK-78282 | Drug Info | Terminated | Inflammatory disease | [2] | |
| Inhibitor | 1-Benzyl-7-chloro-4-hexyloxy-quinolinium | Drug Info | [3] | ||
| 2-Methoxy-N-(3-methyl-2-phenyl-butyl)-benzamide | Drug Info | [4] | |||
| 4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one | Drug Info | [5] | |||
| 5-(4-Phenylbutoxy)psoralen | Drug Info | [6] | |||
| Correloid | Drug Info | [7] | |||
| Correloid derivative | Drug Info | [7] | |||
| CP-339818 | Drug Info | [8] | |||
| Debio-0824 | Drug Info | [9] | |||
| UK-78282 | Drug Info | [8] | |||
| [1-Benzyl-1H-quinolin-(4E)-ylidene]-hexyl-amine | Drug Info | [3] | |||
| Blocker (channel blocker) | 5-(4-phenoxybutoxy)psoralen | Drug Info | [10] | ||
| correolide | Drug Info | [11] | |||
| tetraethylammonium | Drug Info | [12] | |||
| Blocker | Psora-4 | Drug Info | [13] | ||
| Pathways | |||||
| Reactome | Voltage gated Potassium channels | ||||
| WikiPathways | Potassium Channels | ||||
| BDNF signaling pathway | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT02446340) Multiple Ascending Dose Safety Study of ShK-186 (Dalazatide) in Healthy Volunteers. U.S. National Institutes of Health. | ||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009179) | ||||
| REF 3 | J Med Chem. 1995 May 26;38(11):1877-83.Novel inhibitors of potassium ion channels on human T lymphocytes. | ||||
| REF 4 | Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4.Benzamide derivatives as blockers of Kv1.3 ion channel. | ||||
| REF 5 | 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 6 | 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 7 | Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51.Potent Kv1.3 inhibitors from correolide-modification of the C18 position. | ||||
| REF 8 | 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 9 | Durable Pharmacological Responses from the Peptide ShK-186, a Specific Kv1.3 Channel Inhibitor That Suppresses T Cell Mediators of Autoimmune Disease. J Pharmacol Exp Ther. 2012 September; 342(3): 642-653. | ||||
| REF 10 | 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 11 | 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 12 | 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 13 | Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol. 2004 Jun;65(6):1364-74. | ||||
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