Department of Biomedical Sciences, University of Padova, Padova, Italy.
Curr Med Chem. 2013;20(5):671-93. doi: 10.2174/092986713804999312.
Protein kinase CK2 (Casein Kinase 2) is an essential, ubiquitous and highly pleiotropic protein kinase, implicated in several human diseases. In the last decade, several inhibitors of CK2, have been discovered and characterized to be ATP-competitive compounds. However, only one of them, CX-4945, has recently completed Phase I clinical trial as potential anticancer drug. In this review, we report all chemical classes of CK2 inhibitors available in literature, focusing our attention on conventional ATP-competitive and on non ATP-competitive inhibitors, which could represent a new frontier in CK2 inhibition and, consequently, a promising field of study in discovering new drug candidates.
蛋白激酶 CK2（酪蛋白激酶 2）是一种必需的、普遍存在的且具有高度多功能性的蛋白激酶，与多种人类疾病有关。在过去的十年中，已经发现并表征了几种 CK2 的抑制剂，它们都是 ATP 竞争性化合物。然而，最近只有一种抑制剂 CX-4945 作为潜在的抗癌药物完成了 I 期临床试验。在这篇综述中，我们报告了文献中所有可用的 CK2 抑制剂的化学类别，重点关注传统的 ATP 竞争性抑制剂和非 ATP 竞争性抑制剂，它们可能代表 CK2 抑制的一个新前沿，因此也是发现新药物候选物的一个有前途的研究领域。
