Therapeutic Targets Database
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TTD Target ID: TTDC00139

Target Information
NameSerine/threonine protein kinase 12    
Type of targetClinical trial target    
SynonymsAIM-1    
Aurora- and Ipl1-like midbody-associated protein 1    
Aurora-2    
Aurora-2 kinase    
Aurora-B    
Aurora-related kinase 2    
Aurora/IPL1-related kinase 2    
STK-1    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[2]
Solid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[3][4][5]
Drug(s)AZD1152Phase IIAcute Myeloid Leukemia, Haematological malignancies[6]
PHA-739358Phase IICML that relapsed after imatinib or BCR¨CABL-targeted therapy; Metastatic Hormone Refractory Prostate Cancer (MHRPC)[7]
AT-9283Phase I/IIAdult solid tumours, NHL, AML, ALL, CML, MDS and myelofibrosis[7]
AZD1152Phase I/IIMyeloid Leukemia[6]
BI-811283Phase I/IIAML
SNS-314Phase I completedSolid Tumors[8][3][4][5][8]
AMG 900Phase IVarious cancer types
AT9283Phase ILeukemia, Myeloid[9][10]
BI-811283Phase ISolid Tumors
GSK1070916Phase IAdvanced solid tumours[7]
GSK1070916APhase ISolid Tumors
MK-5108Phase ICancer; Neoplasms; Tumors[11][12]
PF-03814735Phase IAdvanced solid tumours[7]
R763Phase IHaematological Malignancies[13]
TAK-901Phase IAdvanced malignancies[14]
VX-689Phase ICancer; Neoplasms; Tumors[7]
CYC-116Terminated in Phase IAdvanced solid tumours[7]
CYC116Terminated in Phase ISolid Tumors[15]
SU-6668DiscontinuedAdvanced solid tumours[16][17]
VX-680Terminated in Phase IChronic Myelogenous Leukemia; Leukemia; Lymphoblastic, Acute, Philadelphia-Positive[16][18]
VX-680Terminated in Phase IILeukemia[16][18]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
UniProt IDQ96GD4
PDB Structure4AF3.    
FunctionMay be directly involved in regulating the cleavage of polar spindle microtubules and is a key regulator for the onset of cytokinesis during mitosis.    
SequenceMAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMEN SSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEH QLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATI MEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYL PPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPTGA QDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA
Related US Patent6,610,677
6,613,776
6,638,926
6,653,300
6,653,301
6,656,939
6,660,731
6,664,247
Target ValidationClick to Find Target Validation Information.    
InhibitorAT-9283[7]
AT9283[9][10]
AZD1152[6]
CYC-116[7]
CYC116[15]
GSK1070916[7]
MK-5108[11][12]
PF-03814735[7]
PHA-739358[7]
R763[13]
SNS-314[8][3][4][5][8]
SU-6668[16][17]
TAK-901[14]
VX-680[16][18]
VX-689[7]
MultitargetAT-9283[7]
AT9283[9][10]
AZD1152[6]
CYC-116[7]
CYC116[15]
GSK1070916[7]
MK-5108[11][12]
PF-03814735[7]
PHA-739358[7]
R763[13]
SNS-314[8][3][4][5][8]
SU-6668[16][17]
VX-680[16][18]
VX-689[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Targeting Aurora-2 kinase in cancer. Mol Cancer Ther. 2003 Jun;2(6):589-95. To Reference
Ref 2The mitotic serine threonine kinase, Aurora-2, is a potential target for drug development in human pancreatic cancer. Mol Cancer Ther. 2004 Apr;3(4):451-7. 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 6AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 7Nat Rev Drug Discov. 2009 Jul;8(7):547-66.Cell cycle kinases as therapeutic targets for cancer. To Reference
Ref 8SNS-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 9Aurora 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 10J 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 11Merck. Product Development Pipeline. July 15 2009. To Reference
Ref 12Merck. Report of Merck. 2009. To Reference
Ref 13J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. To Reference
Ref 14Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 15Report from Cyclacel Pharmaceuticals. Cyclacel Limited. April 2008 To Reference
Ref 16A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 17Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. To Reference
Ref 18Essential roles of mTOR/Akt pathway in Aurora-A cell transformation. Int J Biol Sci. 2009 Jun 19;5(5):444-50. To Reference



 

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