1mp8: Difference between revisions
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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'' | ||