针对催化盒内外的 CK2 抑制剂

Sophie Day-Riley, Rebekah M. West, P. Brear, M. Hyvönen, D. Spring
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引用次数: 0

摘要

CK2 是一种蛋白激酶,在涉及细胞生长、分化、增殖和死亡的众多细胞通路中发挥着重要作用。因此,CK2 的上调与许多疾病类型有关,尤其是癌症。因此,CK2 作为癌症的潜在治疗靶点受到了广泛关注,在过去十年中,已经开发出 40 多种针对 CK2 的化学探针。在本综述中,我们重点介绍了几种针对传统 ATP 结合位点以外位点的化学探针。这些化学探针属于不同的分子类别,从小分子到多肽,具有不同的作用机制。本综述中讨论的许多化学探针都有可能成为选择性靶向 CK2 的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
CK2 Inhibitors Targeting Inside and Outside the Catalytic Box
CK2 is a protein kinase that plays an important role in numerous cellular pathways involved in cell growth, differentiation, proliferation, and death. Consequently, upregulation of CK2 is implicated in many disease types, in particular cancer. As such, CK2 has gained significant attention as a potential therapeutic target in cancer, and over 40 chemical probes targeting CK2 have been developed in the past decade. In this review, we highlighted several chemical probes that target sites outside the conventional ATP-binding site. These chemical probes belong to different classes of molecules, from small molecules to peptides, and possess different mechanisms of action. Many of the chemical probes discussed in this review could serve as promising new candidates for drugs selectively targeting CK2.
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