Department of Molecular Biology, The John Paul II Catholic University of Lublin, ul. Konstantynow 1i, 20-708, Lublin, Poland.
Department of Pharmacognosy, Medical University of Białystok, ul. Mickiewicza 2a, 15-089, Białystok, Poland.
Mol Cell Biochem. 2018 Jul;444(1-2):35-42. doi: 10.1007/s11010-017-3228-1. Epub 2017 Nov 29.
CK2 is a pleiotropic, constitutively active protein kinase responsible for the phosphorylation of more than 300 physiological substrates. Typically, this enzyme is found in tetrameric form consisting of two regulatory subunits CK2β and two catalytic subunits CK2α or CK2α'. Several natural occurring flavonoids were tested for their ability to inhibit both CK2 holoenzymes, CK2αβ and CK2α'β. We identified few substances selectively inhibiting only the α' subunit. Other compounds showed similar effect towards all four isoforms. In some cases, like chrysoeriol, pedalitin, apigenin, and luteolin, the αβ holoenzyme was at least six times better inhibited than the free α subunit. Otherwise, we have found a luteolin derivative decreased the kinase activity of CK2α' with an IC value of 0.8 μM, but the holoenzyme only with 9.5 µM.
CK2 是一种多效、组成型激活的蛋白激酶，负责磷酸化 300 多种生理底物。通常，这种酶以四聚体形式存在，由两个调节亚基 CK2β和两个催化亚基 CK2α或 CK2α'组成。几种天然存在的类黄酮被测试其抑制 CK2 全酶 CK2αβ和 CK2α'β的能力。我们鉴定出一些仅选择性抑制α'亚基的物质。其他化合物对所有四种同工酶表现出相似的效果。在某些情况下，如 chrysoeriol、pedalitin、apigenin 和 luteolin，αβ 全酶的抑制作用至少比游离的α亚基好六倍。否则，我们发现一种木犀草素衍生物以 0.8μM 的 IC 值降低 CK2α'的激酶活性，但全酶仅为 9.5μM。
