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用小分子抑制剂靶向真核延伸因子 2 激酶(eEF2K)治疗癌症。

Targeting eukaryotic elongation factor 2 kinase (eEF2K) with small-molecule inhibitors for cancer therapy.

机构信息

Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.

Nucleic Acid Division, Shanghai Cell Therapy Group, Shanghai 201805, China.

出版信息

Drug Discov Today. 2024 Oct;29(10):104155. doi: 10.1016/j.drudis.2024.104155. Epub 2024 Aug 28.

Abstract

Eukaryotic elongation factor 2 kinase (eEF2K) is a member of the α-kinase family that is activated by calcium/calmodulin. Of note, eEF2K is crucial for regulating translation and is often highly overexpressed in malignant cells. Therefore in this review, we summarize the molecular structure of eEF2K and its oncogenic roles in cancer. Moreover, we further discuss the inhibition of eEF2K with small-molecule inhibitors and other new emerging therapeutic strategies in cancer therapy. Taken together, these inspiring findings provide new insights into a promising strategy for inhibiting eEF2K to greatly improve future cancer therapy.

摘要

真核延伸因子 2 激酶(eEF2K)是钙/钙调蛋白激活的 α-激酶家族的成员。值得注意的是,eEF2K 对于调节翻译至关重要,并且在恶性细胞中常常高度过表达。因此,在这篇综述中,我们总结了 eEF2K 的分子结构及其在癌症中的致癌作用。此外,我们还进一步讨论了用小分子抑制剂和其他新出现的治疗策略抑制 eEF2K 在癌症治疗中的作用。综上所述,这些鼓舞人心的发现为抑制 eEF2K 以极大地改善未来癌症治疗提供了新的思路。

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