Download MendeleyStructural and Mechanistic Basis of the Inhibitory Potency of Selected 2-Aminothiazole Compounds on Protein Kinase CK2.
Lindenblatt, D., Nickelsen, A., Applegate, V.M., Jose, J., Niefind, K.(2020) J Med Chem 63: 7766-7772
- PubMed: 32589844
- DOI: https://doi.org/10.1021/acs.jmedchem.0c00587
- Primary Citation of Related Structures:
6TE2, 6TEI, 6TEW, 6TGU - PubMed Abstract:
Selective inhibitors of protein kinase CK2 with significant cytotoxicity on tumor cells based on a 2-aminothiazole scaffold were described recently. Here, these studies are supplemented with representative CK2α/CK2α' complex structures. They reveal that the 2-aminothiazole-based inhibitors occupy the ATP cavity, whereas preliminary data had indicated an allosteric binding site. The crystal structure findings are corroborated by subsequent enzyme kinetic studies; their atomic-resolution quality provides the basis for future optimization of these promising CK2 inhibitors.
Organizational Affiliation:
Department für Chemie, Institut für Biochemie, Universität zu Köln, Zülpicher Str. 47, D-50674 Köln, Germany.
