Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T77764
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| Former ID |
TTDR01420
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| Target Name |
mRNA of Aurora B
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| Gene Name |
AURKB
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| 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
|
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| Target Type |
Clinical Trial
|
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| Disease | Prostate cancer [ICD9: 185; ICD10: C61] | ||||
| BioChemical Class |
Kinase
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| Target Validation |
T77764
|
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.1
|
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| Sequence |
MAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMEN
SSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEH QLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATI MEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYL PPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPMGA QDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA |
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| Drugs and Mode of Action | |||||
| Drug(s) | PHA-739358 | Drug Info | Phase 2 | Prostate cancer | [1], [2] |
| Inhibitor | 4-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine | Drug Info | [3] | ||
| 4-(4'-Benzamidoanilino)-6,7-dimethoxyquinazoline | Drug Info | [4] | |||
| 6-bromoindirubin-3-oxime | Drug Info | [5] | |||
| 7-bromoindirubin-3-oxime | Drug Info | [5] | |||
| 7-chloroindirubin-3-oxime | Drug Info | [5] | |||
| 7-fluoroindirubin-3-acetoxime | Drug Info | [5] | |||
| 7-fluoroindirubin-3-oxime | Drug Info | [5] | |||
| 7-iodoindirubin-3-oxime | Drug Info | [5] | |||
| CGP-57380 | Drug Info | [6] | |||
| compound 1 | Drug Info | [7] | |||
| compound 10 | Drug Info | [8] | |||
| compound 25 | Drug Info | [9] | |||
| compound 46 | Drug Info | [10] | |||
| HESPERADIN | Drug Info | [10] | |||
| Indirubin-3-acetoxime | Drug Info | [5] | |||
| Indirubin-3-methoxime | Drug Info | [5] | |||
| Indirubin-3-oxime | Drug Info | [5] | |||
| PHA-739358 | Drug Info | [11] | |||
| quinazoline deriv. 1 | Drug Info | [4] | |||
| SU 6656 | Drug Info | [6] | |||
| 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 1 | (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 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025382) | ||||
| REF 3 | Bioorg 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 4 | Proc 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 5 | J 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 6 | Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. | ||||
| REF 7 | A 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 8 | A 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 9 | Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43. | ||||
| REF 10 | J Med Chem. 2006 Feb 9;49(3):955-70.Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. | ||||
| REF 11 | J 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. | ||||
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