使用小分子抑制剂靶向真核延伸因子 2 激酶 (eEF2K) 进行癌症治疗。
Targeting eukaryotic elongation factor 2 kinase (eEF2K) with small-molecule inhibitors for cancer therapy.
发表日期:2024 Aug 28
作者:
Huiping Wang, Wenke Jin, Zixiang Li, Chuanxin Guo, Lan Zhang, Leilei Fu
来源:
DRUG DISCOVERY TODAY
摘要:
真核延伸因子 2 激酶 (eEF2K) 是 α-激酶家族的成员,由钙/钙调蛋白激活。值得注意的是,eEF2K 对于调节翻译至关重要,并且通常在恶性细胞中高度过表达。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,我们进一步讨论了小分子抑制剂对 eEF2K 的抑制以及癌症治疗中其他新兴治疗策略。总而言之,这些鼓舞人心的发现为抑制 eEF2K 的有前途的策略提供了新的见解,从而极大地改善未来的癌症治疗。版权所有 © 2024 Elsevier Ltd. 保留所有权利。
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.Copyright © 2024 Elsevier Ltd. All rights reserved.