2y6o | pdb_00002y6o

Crystal structure of EphA4 kinase domain in complex with Dasatinib.

spinqualitylabelsall models 2y6o, resolution 1.54Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2y6o is a 1 chain structure with sequence from Mus musculus. Full crystallographic information is available from OCA. Ligands: 1N1 Related: 2y6m, 2xyu, 1b0x Activity: Glucokinase, with EC number 2.7.1.2 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed 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. Crystal structure of the EphA4 protein tyrosine kinase domain in the apo- and dasatinib-bound state.,Farenc C, Celie PH, Tensen CP, de Esch IJ, Siegal G FEBS Lett. 2011 Oct 22. PMID:22036717 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

Proteopedia Page Contributors and Editors (what is this?)

OCA