用小分子抑制剂靶向真核细胞延伸因子 2 激酶（eEF2K）治疗癌症。

IF 6.5 2区医学 Q1 PHARMACOLOGY & PHARMACY

Drug Discovery Today Pub Date : 2024-08-28 DOI:10.1016/j.drudis.2024.104155

Huiping Wang , Wenke Jin , Zixiang Li , Chuanxin Guo , Lan Zhang , Leilei Fu

{"title":"用小分子抑制剂靶向真核细胞延伸因子 2 激酶（eEF2K）治疗癌症。","authors":"Huiping Wang , Wenke Jin , Zixiang Li , Chuanxin Guo , Lan Zhang , Leilei Fu","doi":"10.1016/j.drudis.2024.104155","DOIUrl":null,"url":null,"abstract":"<div><p>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.</p></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"29 10","pages":"Article 104155"},"PeriodicalIF":6.5000,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Targeting eukaryotic elongation factor 2 kinase (eEF2K) with small-molecule inhibitors for cancer therapy\",\"authors\":\"Huiping Wang , Wenke Jin , Zixiang Li , Chuanxin Guo , Lan Zhang , Leilei Fu\",\"doi\":\"10.1016/j.drudis.2024.104155\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>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.</p></div>\",\"PeriodicalId\":301,\"journal\":{\"name\":\"Drug Discovery Today\",\"volume\":\"29 10\",\"pages\":\"Article 104155\"},\"PeriodicalIF\":6.5000,\"publicationDate\":\"2024-08-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Discovery Today\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1359644624002800\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Discovery Today","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1359644624002800","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}

引用次数: 0

摘要

真核细胞延伸因子 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 对调节翻译至关重要，在恶性细胞中通常会出现高表达。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小分子抑制剂对 eEF2K 的抑制作用以及其他新兴的癌症治疗策略。总之，这些令人鼓舞的发现为抑制 eEF2K 的前景广阔的策略提供了新的见解，从而大大改善了未来的癌症治疗。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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

查看原文本刊更多论文

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

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.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Drug Discovery Today 医学-药学

CiteScore

14.80

自引率

2.70%

发文量

293

审稿时长

6 months

期刊介绍： Drug Discovery Today delivers informed and highly current reviews for the discovery community. The magazine addresses not only the rapid scientific developments in drug discovery associated technologies but also the management, commercial and regulatory issues that increasingly play a part in how R&D is planned, structured and executed. Features include comment by international experts, news and analysis of important developments, reviews of key scientific and strategic issues, overviews of recent progress in specific therapeutic areas and conference reports.