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PDBsum entry 2y6o
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References listed in PDB file
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Key reference
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Title
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Crystal structure of the epha4 protein tyrosine kinase domain in the apo- And dasatinib-Bound state.
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Authors
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C.Farenc,
P.H.Celie,
C.P.Tensen,
I.J.De esch,
G.Siegal.
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Ref.
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Febs Lett, 2011,
585,
3593-3599.
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PubMed id
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Abstract
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The Eph family of receptor tyrosine kinases regulates diverse cellular processes
while the over-expression of a member of this family, EphA4, has been reported
in a variety of malignant carcinomas. To gain insight into molecular mechanisms
and to facilitate structure-based inhibitor design, we solved the crystal
structure of the native EphA4 kinase domain in both the apo and dasatinib bound
forms. Analysis of the two structures provides insight into structural features
of inhibitor binding and revealed a hydrophobic back-pocket in the ATP- binding
site of EphA4 which was previously unidentified. The structures suggest a route
towards development of novel and specific inhibitors.
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