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2pvj
From Proteopedia
| 2pvj, resolution 1.70Å () | |||||||||
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| Ligands: | |||||||||
| Non-Standard Residues: | |||||||||
| Gene: | ACK2 (Zea mays) | ||||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||||
| Related: | 2pvh, 2pvk, 2pvl, 2pvm, 2pvn
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Contents |
Structure-Based Design of Pyrazolo[1,5-a][1,3,5]triazine Derivatives as Potent Inhibitors of Protein Kinase CK2
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.
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
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
2pvj is a 1 chain structure with sequence from Zea mays. Full crystallographic information is available from OCA.
See Also
Reference
- Nie Z, Perretta C, Erickson P, Margosiak S, Almassy R, Lu J, Averill A, Yager KM, Chu S. Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. Epub 2007 May 18. PMID:17540560 doi:10.1016/j.bmcl.2007.05.041
