Cover Picture: Urolithin as a Converging Scaffold Linking Ellagic acid and Coumarin Analogues: Design of Potent Protein Kinase CK2 Inhibitors (ChemMedChem 12/2011)
✍ Scribed by Dr. Giorgio Cozza; Dr. Alessandra Gianoncelli; Dr. Paolo Bonvini; Dr. Elisa Zorzi; Dr. Riccardo Pasquale; Prof. Angelo Rosolen; Prof.Dr. Lorenzo A. Pinna; Prof. Dr. Flavio Meggio; Prof. Dr. Giuseppe Zagotto; Prof. Dr. Stefano Moro
- Publisher
- John Wiley and Sons
- Year
- 2011
- Tongue
- English
- Weight
- 778 KB
- Volume
- 6
- Category
- Article
- ISSN
- 1860-7179
No coin nor oath required. For personal study only.
✦ Synopsis
The cover picture shows the hypothetical binding motif of a novel potent protein kinase CK2 inhibitor, 4-bromo-3,8-dihydroxy-benzo[c]chromen-6-one, which shows a K i value of 7 nm. CK2 is a ubiquitous, essential, and highly pleiotropic protein kinase, and abnormally high constitutive activity of this enzyme is thought to mediate its pathogenic potential in neoplasia and other diseases, such as viral infections and inflammatory diseases, like glomerulonephritis. Starting from the previous identification of highly active 3,8-dibromo-7-hydroxy-4-methylchromen-2-one and ellagic acid (K i = 20 nm and 60 nm, respectively), an X-ray-driven "cut & paste approach" was applied to design a novel series of urolithins as potent CK2 inhibitors. For more details, see the Full Paper by Stefano Moro et al. on p. 2273 ff.