Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00059

Target Information
NameSerine/threonine-protein kinase 13    
Type of targetClinical trial target    
SynonymsAurora-C    
Aurora/Ipl1-related kinase 3    
Aurora/Ipl1/Eg2 protein 2    
DiseaseLeukemia, Myeloid
[ICD9: 208.9   ICD10: C91-C95]
[1][2]
Solid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[3][4][5]
Drug(s)SNS-314Phase I completedSolid Tumors[6][3][4][5][6]
AMG 900Phase IVarious cancer types
GSK1070916Phase IAdvanced solid tumours[7]
GSK1070916APhase ISolid Tumors
EC NumberEC 2.7.11.1
UniProt IDQ9UQB9
SequenceMSSPRAVVQLGKAQPAGEELATANQTAQQPSSPAMRRLTVDDFEIGRPLGKGKFGNVYLA RLKESHFIVALKVLFKSQIEKEGLEHQLRREIEIQAHLQHPNILRLYNYFHDARRVYLIL EYAPRGELYKELQKSEKLDEQRTATIIEELADALTYCHDKKVIHRDIKPENLLLGFRGEV KIADFGWSVHTPSLRRKTMCGTLDYLPPEMIEGRTYDEKVDLWCIGVLCYELLVGYPPFE SASHSETYRRILKVDVRFPLSMPLGARDLISRLLRYQPLERLPLAQILKHPWVQAHSRRV LPPCAQMAS
Target ValidationClick to Find Target Validation Information.    
Inhibitor6-bromoindirubin-3-oxime[8]
7-bromoindirubin-3-acetoxime[8]
7-bromoindirubin-3-oxime[8]
7-chloroindirubin-3-oxime[8]
7-fluoroindirubin-3-acetoxime[8]
7-fluoroindirubin-3-oxime[8]
7-iodoindirubin-3-oxime[8]
AZD-1152-HQPA,   Barasertib[9]
GSK-1070916[10]
GSK1070916[7]
PHA-680632[11]
SNS-314[6][3][4][5][6]
SU 6656[12]
indirubin-3-acetoxime[8]
indirubin-3-methoxime[8]
indirubin-3-oxime[8]
MultitargetGSK1070916[7]
SNS-314[6][3][4][5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Aurora B kinase inhibition in mitosis: strategies for optimising the use of aurora kinase inhibitors such as AT9283. Cell Cycle. 2009 Jun 15;8(12):1921-9. Epub 2009 Jun 15. To Reference
Ref 2J Med Chem. 2009 Jan 22;52(2):379-88.Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. To Reference
Ref 3The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther. 2009 Apr;8(4):930-9. To Reference
Ref 4Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57. To Reference
Ref 5Water-soluble prodrugs of an Aurora kinase inhibitor. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1409-12. Epub 2009 Jan 19. To Reference
Ref 6SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2009 Aug 1. [Epub ahead of print] To Reference
Ref 7Nat Rev Drug Discov. 2009 Jul;8(7):547-66.Cell cycle kinases as therapeutic targets for cancer. To Reference
Ref 8J Med Chem. 2007 Aug 23;50(17):4027-37. Epub 2007 Aug 1.An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins. To Reference
Ref 9J Med Chem. 2007 May 3;50(9):2213-24. Epub 2007 Mar 21.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. To Reference
Ref 10J Med Chem. 2010 May 27;53(10):3973-4001.Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. To Reference
Ref 11J Med Chem. 2005 Apr 21;48(8):3080-4.Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. To Reference
Ref 12Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. To Reference



 

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