2c6e
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AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH A 5-AMINOPYRIMIDINYL QUINAZOLINE INHIBITOR
OverviewOverview
A novel series of 5-aminopyrimidinyl quinazolines has been developed from, anilino-quinazoline 1, which was identified in a high throughput screen, for Aurora A. Introduction of the pyrimidine ring and optimisation of the, substituents both on this ring and at the C7 position of the quinazoline, led to the discovery of compounds that are highly specific Aurora kinase, inhibitors. Co-crystallisation of one of these inhibitors with a fragment, of Aurora A shows the importance of the benzamido group in achieving, selectivity.
DiseaseDisease
Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]
About this StructureAbout this Structure
2C6E is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . Full crystallographic information is available from OCA.
ReferenceReference
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors., Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. Epub 2005 Dec 5. PMID:16337122
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OCA- Pages with broken file links
- Homo sapiens
- Single protein
- Transferred entry: 2.7.11.1
- Anderson, M.
- Breed, J.
- Mcmiken, H.H.J.
- Pannifer, A.D.
- Pauptit, R.A.
- Rowsell, S.
- HPM
- Atp-binding
- Aurora
- Cancer
- Cell cycle
- Kinase
- Nucleotide-binding
- Phosphorylation
- Serine/threonine-protein kinase
- Transferase
- Transferase/inhibitor complex