2c6e: Difference between revisions
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==Overview== | ==Overview== | ||
A novel series of 5-aminopyrimidinyl quinazolines has been developed from | 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. | ||
==Disease== | ==Disease== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Transferred entry: 2 | [[Category: Transferred entry: 2 7.11 1]] | ||
[[Category: Anderson, M.]] | [[Category: Anderson, M.]] | ||
[[Category: Breed, J.]] | [[Category: Breed, J.]] | ||
[[Category: Mcmiken, H | [[Category: Mcmiken, H H.J.]] | ||
[[Category: Pannifer, A | [[Category: Pannifer, A D.]] | ||
[[Category: Pauptit, R | [[Category: Pauptit, R A.]] | ||
[[Category: Rowsell, S.]] | [[Category: Rowsell, S.]] | ||
[[Category: HPM]] | [[Category: HPM]] | ||
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[[Category: transferase/inhibitor complex]] | [[Category: transferase/inhibitor complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:45:28 2008'' | ||
Revision as of 17:45, 21 February 2008
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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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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
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