Cozza Giorgio, Bonvini Paolo, Zorzi Elisa, Poletto Giorgia, Pagano Mario A, Sarno Stefania, Donella-Deana Arianna, Zagotto Giuseppe, Rosolen Angelo, Pinna Lorenzo A, Meggio Flavio, Moro Stefano
Molecular Modeling Section, Dipartimento di Scienze Farmaceutiche, Università di Padova, via Marzolo 5, Padua, Italy.
J Med Chem. 2006 Apr 20;49(8):2363-6. doi: 10.1021/jm060112m.
Casein kinase 2 (CK2) is a ubiquitous, essential, and highly pleiotropic protein kinase whose abnormally high constitutive activity is suspected to underlie its pathogenic potential in neoplasia and other diseases. Using a virtual screening approach, we have identified the ellagic acid, a naturally occurring tannic acid derivative, as a novel potent CK2 inhibitor. At present, ellagic acid represents the most potent known CK2 inhibitor (K(i) = 20 nM).
酪蛋白激酶2（CK2）是一种普遍存在、不可或缺且具有高度多效性的蛋白激酶，其异常高的组成性活性被怀疑是其在肿瘤和其他疾病中致病潜力的基础。通过虚拟筛选方法，我们鉴定出了一种天然存在的单宁酸衍生物——鞣花酸，它是一种新型的强效CK2抑制剂。目前，鞣花酸是已知最有效的CK2抑制剂（抑制常数K(i)=20 nM）。
