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选定的类黄酮化合物有望成为蛋白激酶CK2α和CK2α'(CK2的催化亚基)的抑制剂。

Selected flavonoid compounds as promising inhibitors of protein kinase CK2α and CK2α', the catalytic subunits of CK2.

作者信息

Baier Andrea, Galicka Anna, Nazaruk Jolanta, Szyszka Ryszard

机构信息

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.

出版信息

Phytochemistry. 2017 Apr;136:39-45. doi: 10.1016/j.phytochem.2016.12.018. Epub 2016 Dec 30.

Abstract

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.

摘要

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。

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