2c6e
From Proteopedia
(New page: 200px<br /> <applet load="2c6e" size="450" color="white" frame="true" align="right" spinBox="true" caption="2c6e, resolution 2.1Å" /> '''AURORA A KINASE ACTI...) |
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==About this Structure== | ==About this Structure== | ||
| - | 2C6E is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with HPM as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C6E OCA]]. | + | 2C6E is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with HPM as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C6E OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| + | [[Category: Transferred entry: 2.7.11.1]] | ||
[[Category: Anderson, M.]] | [[Category: Anderson, M.]] | ||
[[Category: Breed, J.]] | [[Category: Breed, J.]] | ||
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[[Category: transferase/inhibitor complex]] | [[Category: transferase/inhibitor complex]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:29:01 2007'' |
Revision as of 09:24, 30 October 2007
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AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH A 5-AMINOPYRIMIDINYL QUINAZOLINE INHIBITOR
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.
About this Structure
2C6E is a [Single protein] structure of sequence from [Homo sapiens] with HPM as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. 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 Tue Oct 30 11:29:01 2007
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. | HPM | Atp-binding | Aurora | Cancer | Cell cycle | Kinase | Nucleotide-binding | Phosphorylation | Serine/threonine-protein kinase | Transferase | Transferase/inhibitor complex
