2pvh
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Revision as of 08:21, 14 May 2008
Structure-Based Design of Pyrazolo[1,5-a][1,3,5]triazine Derivatives as Potent Inhibitors of Protein Kinase CK2
Overview
The structure-based design, synthesis, and anticancer activity of novel inhibitors of protein kinase CK2 are described. Using pyrazolo[1,5-a][1,3,5]triazine as the core scaffold, a structure-guided series of modifications provided pM inhibitors with microM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.
About this Structure
2PVH is a Single protein structure of sequence from Zea mays. Full crystallographic information is available from OCA.
Reference
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2., Nie Z, Perretta C, Erickson P, Margosiak S, Almassy R, Lu J, Averill A, Yager KM, Chu S, Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. Epub 2007 May 18. PMID:17540560 Page seeded by OCA on Wed May 14 11:21:22 2008
Categories: Non-specific serine/threonine protein kinase | Single protein | Zea mays | Almassy, R. | Averill, A. | Chu, S. | Erickson, P. | Lu, J. | Margosiak, S. | Nie, Z. | Perretta, C. | Yager, K M. | Casein kinase ii | Enzyme-inhibitor complex | Protein kinase ck2 | Structure-based drug design | Transferase
