1mp8
From Proteopedia
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==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. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
| - | [[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 G.]] |
[[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: tyrosine protein kinase]] | [[Category: tyrosine protein kinase]] | ||
| - | ''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 13:57:37 2008'' |
Revision as of 11:57, 21 February 2008
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Crystal structure of Focal Adhesion Kinase (FAK)
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.
About this Structure
1MP8 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 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 13:57:37 2008
