Baier Andrea, Galicka Anna, Nazaruk Jolanta, Szyszka Ryszard
Department of Molecular Biology, The John Paul II Catholic University of Lublin, ul. Konstantynów 1i, 20-708 Lublin, Poland.
Department of Medical Chemistry, Medical University of Białystok, ul. Mickiewicza 2a, 15-089 Białystok, Poland.
Phytochemistry. 2017 Apr;136:39-45. doi: 10.1016/j.phytochem.2016.12.018. Epub 2016 Dec 30.
CK2 is a ubiquitous protein kinase involved in many cell functions. During the last years it became an interesting target in cancer research. A series of flavonoid compounds was tested as inhibitors of protein kinase CK2. Several substances were found to be highly active against both catalytic subunits with IC values below 1 μM in case of CK2α'. The most promising inhibitor we identified is chrysoeriol with IC values of 250 and 34 nM for CK2α and CK2α', respectively.
CK2是一种参与多种细胞功能的普遍存在的蛋白激酶。在过去几年中,它成为癌症研究中一个有趣的靶点。一系列黄酮类化合物作为蛋白激酶CK2的抑制剂进行了测试。发现几种物质对两个催化亚基都具有高活性,对于CK2α',其IC值低于1μM。我们鉴定出的最有前景的抑制剂是白杨黄素,其对CK2α和CK2α'的IC值分别为250 nM和34 nM。