2c6d
From Proteopedia
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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: ANP]] | [[Category: ANP]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''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 16:45:25 2008'' |
Revision as of 14:45, 21 February 2008
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AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH ADPNP
Contents |
Overview
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
Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]
About this Structure
2C6D is a Single protein structure of sequence from Homo sapiens with , and as ligands. 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.
Reference
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
Page seeded by OCA on Thu Feb 21 16:45:25 2008
Categories: 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. | ANP | GOL | PO4 | Atp-binding | Aurora | Cancer | Cell cycle | Kinase | Mitosis | Nucleotide-binding | Phosphorylation | Serine/threonine-protein kinase | Transferase
