Target Information
Target General Infomation | |||||
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Target ID |
T51565
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Former ID |
TTDR00257
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Target Name |
Casein kinase II, alpha chain
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Gene Name |
CSNK2A1
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Synonyms |
CK II; Protein kinase CK2; CK II alpha; Casein kinase II subunit alpha; CSNK2A1
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Target Type |
Discontinued
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Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
Function |
Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. The alpha and alpha' chains contain the catalytic site. Participates in wnt signaling.
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BioChemical Class |
Kinase
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Target Validation |
T51565
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UniProt ID | |||||
EC Number |
EC 2.7.1.37
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Sequence |
MSGPVPSRARVYTDVNTHRPREYWDYESHVVEWGNQDDYQLVRKLGRGKYSEVFEAINIT
NNEKVVVKILKPVKKKKIKREIKILENLRGGPNIITLADIVKDPVSRTPALVFEHVNNTD FKQLYQTLTDYDIRFYMYEILKALDYCHSMGIMHRDVKPHNVMIDHEHRKLRLIDWGLAE FYHPGQEYNVRVASRYFKGPELLVDYQMYDYSLDMWSLGCMLASMIFRKEPFFHGHDNYD QLVRIAKVLGTEDLYDYIDKYNIELDPRFNDILGRHSRKRWERFVHSENQHLVSPEALDF LDKLLRYDHQSRLTAREAMEHPYFYTVVKDQARMGSSSMPGGSTPVSSANMMSGISSVPT PSPLGPLAGSPVIAAANPLGMPVPAAAGAQQ |
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Structure |
1JWH; 1NA7; 1PJK; 2PVR; 2ZJW; 3AMY; 3AT2; 3AT3; 3AT4; 3AXW; 3BQC; 3C13; 3FWQ; 3H30; 3JUH; 3MB6; 3MB7; 3NGA; 3NSZ; 3OWJ; 3OWK; 3OWL; 3PE1; 3PE2; 3PE4; 3Q04; 3Q9W; 3Q9X; 3Q9Y; 3Q9Z; 3QA0; 3R0T; 3RPS; 3TAX; 3U4U; 3U87; 3U9C; 3W8L; 3WAR; 3WIK; 3WIL; 4BXA; 4BXB; 4DGL; 4FBX; 4GRB; 4GUB; 4GYW; 4GYY; 4GZ3; 4IB5; 4KWP; 4MD7; 4MD8; 4MD9; 4NH1; 4RLL; 1JWH; 1NA7; 1PJK; 2PVR; 2ZJW; 3BQC; 3BW5; 3C13
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Drugs and Mode of Action | |||||
Inhibitor | 4,5,6,7-tetrabromo-1H-benzimidazole | Drug Info | [529933] | ||
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole | Drug Info | [530101] | |||
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | [528490] | |||
5,6,8-trichloroquinoline-4-one-3-carboxylic acid | Drug Info | [528489] | |||
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole | Drug Info | [530101] | |||
7,8-dichloroquinoline-4-one-3-carboxylic acid | Drug Info | [528489] | |||
AdoC(Dpr)2AlaArg6 | Drug Info | [525511] | |||
APIGENIN | Drug Info | [530101] | |||
BALANOL | Drug Info | [534297] | |||
CGP-029482 | Drug Info | [530101] | |||
compound 1a | Drug Info | [532826] | |||
compound 2c | Drug Info | [531713] | |||
CX-5011 | Drug Info | [543439] | |||
CX-7000 | Drug Info | [543439] | |||
ELLAGIC ACID | Drug Info | [530101] | |||
EMODIN | Drug Info | [530101] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Ribosome biogenesis in eukaryotes | ||||
NF-kappa B signaling pathway | |||||
Wnt signaling pathway | |||||
Adherens junction | |||||
Tight junction | |||||
Measles | |||||
Herpes simplex infection | |||||
Epstein-Barr virus infection | |||||
NetPath Pathway | FSH Signaling Pathway | ||||
Pathway Interaction Database | BCR signaling pathway | ||||
Atypical NF-kappaB pathway | |||||
DNA-PK pathway in nonhomologous end joining | |||||
Presenilin action in Notch and Wnt signaling | |||||
Role of Calcineurin-dependent NFAT signaling in lymphocytes | |||||
E-cadherin signaling in the nascent adherens junction | |||||
Lissencephaly gene (LIS1) in neuronal migration and development | |||||
PDGFR-alpha signaling pathway | |||||
Signaling mediated by p38-alpha and p38-beta | |||||
Alpha-synuclein signaling | |||||
Reactome | Condensation of Prometaphase Chromosomes | ||||
WikiPathways | Mitotic Prometaphase | ||||
BDNF signaling pathway | |||||
TNF alpha Signaling Pathway | |||||
L1CAM interactions | |||||
References | |||||
Ref 542983 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8142). | ||||
Ref 525511 | Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases. | ||||
Ref 528489 | J Med Chem. 2006 Nov 2;49(22):6443-50.Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2. | ||||
Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
Ref 529933 | Bioorg Med Chem. 2009 Feb 15;17(4):1573-8. Epub 2009 Jan 7.Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2. | ||||
Ref 530101 | Bioorg Med Chem Lett. 2009 Jun 1;19(11):2920-3. Epub 2009 Apr 22.Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid. | ||||
Ref 531713 | CK2alpha and CK2alpha' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives. Eur J Med Chem. 2012 Jan;47(1):345-50. | ||||
Ref 532826 | Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett. 2013 Jul 3;4(8):800-5. |
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