1muo
From Proteopedia
(New page: 200px<br /> <applet load="1muo" size="450" color="white" frame="true" align="right" spinBox="true" caption="1muo, resolution 2.9Å" /> '''CRYSTAL STRUCTURE OF...) |
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| - | [[Image:1muo.gif|left|200px]]<br /> | + | [[Image:1muo.gif|left|200px]]<br /><applet load="1muo" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1muo" size=" | + | |
caption="1muo, resolution 2.9Å" /> | caption="1muo, resolution 2.9Å" /> | ||
'''CRYSTAL STRUCTURE OF AURORA-2, AN ONCOGENIC SERINE-THREONINE KINASE'''<br /> | '''CRYSTAL STRUCTURE OF AURORA-2, AN ONCOGENIC SERINE-THREONINE KINASE'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Aurora-2 is a key member of a closely related subgroup of serine/threonine | + | Aurora-2 is a key member of a closely related subgroup of serine/threonine kinases that plays important roles in the completion of essential mitotic events. Aurora-2 is oncogenic and amplified in various human cancers and could be an important therapeutic target for inhibitory molecules that would disrupt the cell cycle and block proliferation. We report the first crystal structure of Aurora-2 kinase in complex with adenosine. Analysis of residues in the active site suggests differences with structurally and biologically related protein kinases. The activation loop, which contains residues specific to the Aurora family of kinases, has a unique conformation. These results provide valuable insight into the design of selective and highly potent ATP-competitive inhibitors of the Aurora kinases. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1MUO 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 ADN as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1MUO 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 <scene name='pdbligand=ADN:'>ADN</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MUO OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Austen, D | + | [[Category: Austen, D A.]] |
| - | [[Category: Cheetham, G | + | [[Category: Cheetham, G M.T.]] |
| - | [[Category: Coll, J | + | [[Category: Coll, J T.]] |
| - | [[Category: Knegtel, R | + | [[Category: Knegtel, R M.A.]] |
| - | [[Category: Lippke, J | + | [[Category: Lippke, J A.]] |
| - | [[Category: Renwick, S | + | [[Category: Renwick, S B.]] |
[[Category: Swenson, L.]] | [[Category: Swenson, L.]] | ||
[[Category: Weber, P.]] | [[Category: Weber, P.]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:59:10 2008'' |
Revision as of 11:59, 21 February 2008
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CRYSTAL STRUCTURE OF AURORA-2, AN ONCOGENIC SERINE-THREONINE KINASE
Contents |
Overview
Aurora-2 is a key member of a closely related subgroup of serine/threonine kinases that plays important roles in the completion of essential mitotic events. Aurora-2 is oncogenic and amplified in various human cancers and could be an important therapeutic target for inhibitory molecules that would disrupt the cell cycle and block proliferation. We report the first crystal structure of Aurora-2 kinase in complex with adenosine. Analysis of residues in the active site suggests differences with structurally and biologically related protein kinases. The activation loop, which contains residues specific to the Aurora family of kinases, has a unique conformation. These results provide valuable insight into the design of selective and highly potent ATP-competitive inhibitors of the Aurora kinases.
Disease
Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]
About this Structure
1MUO is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
Reference
Crystal structure of aurora-2, an oncogenic serine/threonine kinase., Cheetham GM, Knegtel RM, Coll JT, Renwick SB, Swenson L, Weber P, Lippke JA, Austen DA, J Biol Chem. 2002 Nov 8;277(45):42419-22. Epub 2002 Sep 16. PMID:12237287
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