2c6d: Difference between revisions
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[[Image:2c6d.gif|left|200px]]<br /> | [[Image:2c6d.gif|left|200px]]<br /><applet load="2c6d" size="450" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2c6d" size="450" color="white" frame="true" align="right" spinBox="true" | |||
caption="2c6d, resolution 2.2Å" /> | caption="2c6d, resolution 2.2Å" /> | ||
'''AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH ADPNP'''<br /> | '''AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH ADPNP'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
2C6D 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 PO4, ANP and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. 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] | 2C6D 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 PO4, ANP and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. 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] Known structural/functional Site: <scene name='pdbsite=AC1:Anp Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C6D OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
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Revision as of 20:01, 18 December 2007
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AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH ADPNP
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
2C6D is a Single protein structure of sequence from Homo sapiens with PO4, ANP and GOL 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.
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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