CK2 in Cancer: Cellular and Biochemical Mechanisms and Potential Therapeutic Target.
CK2 in Cancer: Cellular and Biochemical Mechanisms and Potential Therapeutic Target.
复制标题
DOI：
10.3390/ph10010018
复制
发表时间：
2017-01-28
期刊：
影响因子：
--
通讯作者：
Dominguez I
中科院分区：
文献类型：
--
作者：
Chua MM;Ortega CE;Sheikh A;Lee M;Abdul-Rassoul H;Hartshorn KL;Dominguez I
CK2基因在许多人类癌症中过表达，并且大多数情况下过表达与更差的预后相关。小鼠中的位点特异性表达导致癌症发展（例如，乳腺癌、淋巴瘤），表明CK2的致癌性质。CK2参与癌症的许多关键方面，包括细胞凋亡的抑制、信号通路的调节、DNA损伤反应和细胞周期调节。现在有许多CK2抑制剂可供使用，并已在体外和临床前模型中显示出对各种癌症具有活性。其中一些抑制剂目前也正在临床试验中进行探索。在这篇综述中，我们将研究一些主要的癌症，其中CK2抑制剂有希望在体外和临床前研究的基础上，提出的细胞和信号传导机制的抗癌活性的CK2抑制剂，和当前或最近的临床试验使用CK2抑制剂。
CK2 genes are overexpressed in many human cancers, and most often overexpression is associated with worse prognosis. Site-specific expression in mice leads to cancer development (e.g., breast, lymphoma) indicating the oncogenic nature of CK2. CK2 is involved in many key aspects of cancer including inhibition of apoptosis, modulation of signaling pathways, DNA damage response, and cell cycle regulation. A number of CK2 inhibitors are now available and have been shown to have activity against various cancers in vitro and in pre-clinical models. Some of these inhibitors are now undergoing exploration in clinical trials as well. In this review, we will examine some of the major cancers in which CK2 inhibition has promise based on in vitro and pre-clinical studies, the proposed cellular and signaling mechanisms of anti-cancer activity by CK2 inhibitors, and the current or recent clinical trials using CK2 inhibitors.