Target Information

Target General Infomation
Target ID
T77764
Former ID
TTDR01420
Target Name
mRNA of Aurora B
Gene Name
AURKB
Synonyms
AIM1 (mRNA); ARK2 (mRNA); Aurora 1 (mRNA); Aurora and IPL1like midbodyassociated protein 1 (mRNA); Aurora kinase B (mRNA); Aurora/IPL1related kinase 2 (mRNA); Aurorarelated kinase 2 (mRNA); STK1 (mRNA); Serine/threonineprotein kinase 12 (mRNA); Serine/threonineprotein kinase 5 (mRNA); Serine/threonineprotein kinase auroraB (mRNA); AURKB
Target Type
Clinical Trial
Disease Prostate cancer [ICD9: 185; ICD10: C61]
BioChemical Class
Kinase
Target Validation
T77764
UniProt ID
Q96GD4
EC Number
EC 2.7.11.1
Sequence
MAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMEN
SSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEH
QLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATI
MEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYL
PPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPMGA
QDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA
Drugs and Mode of Action
Drug(s) PHA-739358 Drug Info Phase 2 Prostate cancer [542852], [548410]
Inhibitor 4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine Drug Info [530806]
4-(4'-Benzamidoanilino)-6,7-dimethoxyquinazoline Drug Info [529213]
6-bromoindirubin-3-oxime Drug Info [528968]
7-bromoindirubin-3-oxime Drug Info [528968]
7-chloroindirubin-3-oxime Drug Info [528968]
7-fluoroindirubin-3-acetoxime Drug Info [528968]
7-fluoroindirubin-3-oxime Drug Info [528968]
7-iodoindirubin-3-oxime Drug Info [528968]
CGP-57380 Drug Info [529039]
compound 1 Drug Info [532161]
compound 10 Drug Info [530097]
compound 25 Drug Info [531168]
compound 46 Drug Info [528000]
HESPERADIN Drug Info [528000]
Indirubin-3-acetoxime Drug Info [528968]
Indirubin-3-methoxime Drug Info [528968]
Indirubin-3-oxime Drug Info [528968]
PHA-739358 Drug Info [527513]
quinazoline deriv. 1 Drug Info [529213]
SU 6656 Drug Info [529039]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Pathway Interaction Database Aurora B signaling
Signaling by Aurora kinases
Aurora C signaling
FOXM1 transcription factor network
Aurora A signaling
Reactome Cdh1 targeted proteins in late mitosis/early G1
Separation of Sister Chromatids
Resolution of Sister Chromatid Cohesion
RHO GTPases Activate Formins
Mitotic Prometaphase
WikiPathways Mitotic Metaphase and Anaphase
Mitotic Prometaphase
Regulation of Microtubule Cytoskeleton
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
APC/C-mediated degradation of cell cycle proteins
References
Ref 542852(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: 7937).
Ref 548410Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025382)
Ref 527513J 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.
Ref 528000J Med Chem. 2006 Feb 9;49(3):955-70.Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Ref 528968J 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.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 529213Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Ref 530097A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem. 2009 May 28;52(10):3300-7.
Ref 530806Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5. Epub 2010 Mar 1.Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.
Ref 531168Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43.
Ref 532161A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038. Epub 2012 Oct 22.
Ref 549671US patent application no. 7,375,212, Modulation of Aurora B expression.

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