4rlk | pdb_00004rlk

Crystal structure of Z. mays CK2alpha in complex with the ATP-competitive inhibitor 4-[(E)-(fluoren-9-ylidenehydrazinylidene)-methyl] benzoate

spinqualitylabelsall models 4rlk, resolution 1.24Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4rlk is a 1 chain structure with sequence from Zea mays. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.24Å Ligands: ACT, E91, GOL Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CSK2A_MAIZE Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. The alpha chain contains the catalytic site. Publication Abstract from PubMed Screening for protein kinase CK2 inhibitors of the structural diversity compound library (DTP NCI/NIH) led to the discovery of 4-[(E)-(fluoren-9-ylidenehydrazinylidene)-methyl]benzoic acid (E9). E9 induces apoptotic cell death in various cancer cell lines and upon hypoxia, the compound suppresses CK2-catalyzed HSP90/Cdc37 phosphorylation and induces HIF-1alpha degradation. Furthermore, E9 exerts a strong anti-tumour activity by inducing necrosis in murine xenograft models underlining its potential to be used for cancer treatment in future clinical studies. Crystal structure analysis of human and maize CK2alpha in complex with E9 reveals unique binding properties of the inhibitor to the enzyme, accounting for its affinity and selectivity. Protein kinase CK2 inhibition is associated with the destabilization of HIF-1alpha in human cancer cells.,Guerra B, Rasmussen TD, Schnitzler A, Jensen HH, Boldyreff BS, Miyata Y, Marcussen N, Niefind K, Issinger OG Cancer Lett. 2015 Jan 28;356(2 Pt B):751-61. doi: 10.1016/j.canlet.2014.10.026., Epub 2014 Oct 28. PMID:25449433 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Casein kinase 3D structures

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