On July 15, 2018, Brear, Paul; North, Andrew; Iegre, Jessica; Hadje Georgiou, Kathy; Lubin, Alexandra; Carro, Laura; Green, William; Sore, Hannah F.; Hyvonen, Marko; Spring, David R. published an article.Reference of 3-Acetyldihydrofuran-2(3H)-one The title of the article was Novel non-ATP competitive small molecules targeting the CK2 α/β interface. And the article contained the following:
Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell-signaling pathways, this makes it a prime target for down regulation to fight tumor growth. Herein, we report a fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the holoenzyme. A fragment, CAM187, with an IC50 of 44μM and a mol. weight of only 257gmol-1 has been identified as the most promising compound Importantly, the lead fragment only bound at the interface and was not observed in the ATP binding site of the protein when co-crystallized with CK2α. The fragment-like mols. discovered in this study represent unique scaffolds to CK2 inhibition and leave room for further optimization. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Reference of 3-Acetyldihydrofuran-2(3H)-one
The Article related to preparation nonatp targeting ck2 alpha beta, ck2, fragment based drug discovery, protein-protein interaction, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Reference of 3-Acetyldihydrofuran-2(3H)-one
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