Target Information

Target General Infomation
Target ID
T76914
Former ID
TTDR00903
Target Name
Potassium voltage-gated channel subfamily A member 3
Gene Name
KCNA3
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
Target Type
Clinical Trial
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.
BioChemical Class
Voltage-gated ion channel
Target Validation
T76914
UniProt ID
P22001
Sequence
MDERLSLLRSPPPPSARHRAHPPQRPASSGGAHTLVNHGYAEPAAGRELPPDMTVVPGDH
LLEPEVADGGGAPPQGGCGGGGCDRYEPLPPSLPAAGEQDCCGERVVINISGLRFETQLK
TLCQFPETLLGDPKRRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRIRRPVNVPIDIF
SEEIRFYQLGEEAMEKFREDEGFLREEERPLPRRDFQRQVWLLFEYPESSGPARGIAIVS
VLVILISIVIFCLETLPEFRDEKDYPASTSQDSFEAAGNSTSGSRAGASSFSDPFFVVET
LCIIWFSFELLVRFFACPSKATFSRNIMNLIDIVAIIPYFITLGTELAERQGNGQQAMSL
AILRVIRLVRVFRIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAE
ADDPTSGFSSIPDAFWWAVVTMTTVGYGDMHPVTIGGKIVGSLCAIAGVLTIALPVPVIV
SNFNYFYHRETEGEEQSQYMHVGSCQHLSSSAEELRKARSNSTLSKSEYMVIEEGGMNHS
AFPQTPFKTGNSTATCTTNNNPNSCVNIKKIFTDV
Drugs and Mode of Action
Drug(s) Debio-0824 Drug Info Phase 1 Psoriatic arthritis [525193]
UK-78282 Drug Info Terminated Inflammatory disease [546612]
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
Reactome Voltage gated Potassium channels
WikiPathways Potassium Channels
BDNF signaling pathway
References
Ref 525193ClinicalTrials.gov (NCT02446340) Multiple Ascending Dose Safety Study of ShK-186 (Dalazatide) in Healthy Volunteers. U.S. National Institutes of Health.
Ref 546612Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009179)
Ref 525474Identification 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 526035J 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 526574Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4.Benzamide derivatives as blockers of Kv1.3 ion channel.
Ref 527342Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51.Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Ref 527687Design 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 531233Bioorg 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 531235Bioorg 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 533612Pharmacological 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 533627J Med Chem. 1995 May 26;38(11):1877-83.Novel inhibitors of potassium ion channels on human T lymphocytes.
Ref 535968Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol. 2004 Jun;65(6):1364-74.
Ref 544248Durable 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.

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