Target Information

Target General Infomation
Target ID
T51565
Former ID
TTDR00257
Target Name
Casein kinase II, alpha chain
Gene Name
CSNK2A1
Synonyms
CK II; Protein kinase CK2; CK II alpha; Casein kinase II subunit alpha; CSNK2A1
Target Type
Discontinued
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.
BioChemical Class
Kinase
Target Validation
T51565
UniProt ID
P68400
EC Number
EC 2.7.1.37
Sequence
MSGPVPSRARVYTDVNTHRPREYWDYESHVVEWGNQDDYQLVRKLGRGKYSEVFEAINIT
NNEKVVVKILKPVKKKKIKREIKILENLRGGPNIITLADIVKDPVSRTPALVFEHVNNTD
FKQLYQTLTDYDIRFYMYEILKALDYCHSMGIMHRDVKPHNVMIDHEHRKLRLIDWGLAE
FYHPGQEYNVRVASRYFKGPELLVDYQMYDYSLDMWSLGCMLASMIFRKEPFFHGHDNYD
QLVRIAKVLGTEDLYDYIDKYNIELDPRFNDILGRHSRKRWERFVHSENQHLVSPEALDF
LDKLLRYDHQSRLTAREAMEHPYFYTVVKDQARMGSSSMPGGSTPVSSANMMSGISSVPT
PSPLGPLAGSPVIAAANPLGMPVPAAAGAQQ
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
Drugs and Mode of Action
Drug(s) BALANOL Drug Info Terminated Discovery agent [542983], [545589]
EMODIN Drug Info Terminated Discovery agent [546328]
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 545589Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003814)
Ref 546328Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007489)
Ref 525511Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.
Ref 528489J Med Chem. 2006 Nov 2;49(22):6443-50.Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2.
Ref 528490J 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 529933Bioorg 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 530101Bioorg 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 531713CK2alpha 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 532826Structure 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.
Ref 534297J Med Chem. 1996 Dec 20;39(26):5215-27.Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Ref 543439(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. (Target id: 1549).

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