1mq4
From Proteopedia
(New page: 200px<br /> <applet load="1mq4" size="450" color="white" frame="true" align="right" spinBox="true" caption="1mq4, resolution 1.90Å" /> '''Crystal Structure o...) |
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| - | [[Image:1mq4.gif|left|200px]]<br /> | + | [[Image:1mq4.gif|left|200px]]<br /><applet load="1mq4" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1mq4" size=" | + | |
caption="1mq4, resolution 1.90Å" /> | caption="1mq4, resolution 1.90Å" /> | ||
'''Crystal Structure of Aurora-A Protein Kinase'''<br /> | '''Crystal Structure of Aurora-A Protein Kinase'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Protein kinases are important drug targets in human cancers, inflammation, and metabolic diseases. This report presents the structures of kinase | + | Protein kinases are important drug targets in human cancers, inflammation, and metabolic diseases. This report presents the structures of kinase domains for three cancer-associated protein kinases: ephrin receptor A2 (EphA2), focal adhesion kinase (FAK), and Aurora-A. The expression profiles of EphA2, FAK, and Aurora-A in carcinomas suggest that inhibitors of these kinases may have inherent potential as therapeutic agents. The structures were determined from crystals grown in nanovolume droplets, which produced high-resolution diffraction data at 1.7, 1.9, and 2.3 A for FAK, Aurora-A, and EphA2, respectively. The FAK and Aurora-A structures are the first determined within two unique subfamilies of human kinases, and all three structures provide new insights into kinase regulation and the design of selective inhibitors. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1MQ4 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 MG, PO4 and ADP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1MQ4 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=MG:'>MG</scene>, <scene name='pdbligand=PO4:'>PO4</scene> and <scene name='pdbligand=ADP:'>ADP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MQ4 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Cronin, C | + | [[Category: Cronin, C N.]] |
| - | [[Category: Knuth, M | + | [[Category: Knuth, M W.]] |
| - | [[Category: McRee, D | + | [[Category: McRee, D E.]] |
[[Category: Nelson, C.]] | [[Category: Nelson, C.]] | ||
[[Category: Nowakowski, J.]] | [[Category: Nowakowski, J.]] | ||
| - | [[Category: Pavletich, N | + | [[Category: Pavletich, N P.]] |
[[Category: Rodgers, J.]] | [[Category: Rodgers, J.]] | ||
| - | [[Category: Sang, B | + | [[Category: Sang, B C.]] |
| - | [[Category: Scheibe, D | + | [[Category: Scheibe, D N.]] |
| - | [[Category: Swanson, R | + | [[Category: Swanson, R V.]] |
| - | [[Category: Thompson, D | + | [[Category: Thompson, D A.]] |
[[Category: ADP]] | [[Category: ADP]] | ||
[[Category: MG]] | [[Category: MG]] | ||
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[[Category: protein kinase structure]] | [[Category: protein kinase structure]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:57:50 2008'' |
Revision as of 11:57, 21 February 2008
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Crystal Structure of Aurora-A Protein Kinase
Contents |
Overview
Protein kinases are important drug targets in human cancers, inflammation, and metabolic diseases. This report presents the structures of kinase domains for three cancer-associated protein kinases: ephrin receptor A2 (EphA2), focal adhesion kinase (FAK), and Aurora-A. The expression profiles of EphA2, FAK, and Aurora-A in carcinomas suggest that inhibitors of these kinases may have inherent potential as therapeutic agents. The structures were determined from crystals grown in nanovolume droplets, which produced high-resolution diffraction data at 1.7, 1.9, and 2.3 A for FAK, Aurora-A, and EphA2, respectively. The FAK and Aurora-A structures are the first determined within two unique subfamilies of human kinases, and all three structures provide new insights into kinase regulation and the design of selective inhibitors.
Disease
Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]
About this Structure
1MQ4 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Full crystallographic information is available from OCA.
Reference
Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography., Nowakowski J, Cronin CN, McRee DE, Knuth MW, Nelson CG, Pavletich NP, Rogers J, Sang BC, Scheibe DN, Swanson RV, Thompson DA, Structure. 2002 Dec;10(12):1659-67. PMID:12467573
Page seeded by OCA on Thu Feb 21 13:57:50 2008
