锰酸盐抑制剂:专利审查。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY
Pharmaceutical patent analyst Pub Date : 2021-01-01 Epub Date: 2021-01-14 DOI:10.4155/ppa-2020-0028
Ahmed M Abdelaziz, Mingfeng Yu, Shudong Wang
{"title":"锰酸盐抑制剂:专利审查。","authors":"Ahmed M Abdelaziz,&nbsp;Mingfeng Yu,&nbsp;Shudong Wang","doi":"10.4155/ppa-2020-0028","DOIUrl":null,"url":null,"abstract":"<p><p>The alteration of mRNA translation has a crucial role in defining the changes in cellular proteome. The phosphorylation of eukaryotic initiation factor 4E by mitogen-activated protein kinase-interacting kinases (Mnks) leads to the release and translation of mRNAs of specific oncogenic proteins. In recent years, the efforts made by the pharmaceutical industry to develop novel chemical skeletons to create potent and selective Mnk inhibitors have been fruitful. The pyridone-aminal scaffold has been utilized to generate several series of Mnk inhibitors presented in multiple patent applications and research articles. Tomivosertib (eFT508) is one of the molecules with such scaffold. It is one of the first two Mnk inhibitors that entered clinical trials, and has displayed momentous activity against several solid and hematological cancers. The present compilation provides a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.8000,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"8","resultStr":"{\"title\":\"Mnk inhibitors: a patent review.\",\"authors\":\"Ahmed M Abdelaziz,&nbsp;Mingfeng Yu,&nbsp;Shudong Wang\",\"doi\":\"10.4155/ppa-2020-0028\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The alteration of mRNA translation has a crucial role in defining the changes in cellular proteome. The phosphorylation of eukaryotic initiation factor 4E by mitogen-activated protein kinase-interacting kinases (Mnks) leads to the release and translation of mRNAs of specific oncogenic proteins. In recent years, the efforts made by the pharmaceutical industry to develop novel chemical skeletons to create potent and selective Mnk inhibitors have been fruitful. The pyridone-aminal scaffold has been utilized to generate several series of Mnk inhibitors presented in multiple patent applications and research articles. Tomivosertib (eFT508) is one of the molecules with such scaffold. It is one of the first two Mnk inhibitors that entered clinical trials, and has displayed momentous activity against several solid and hematological cancers. The present compilation provides a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years.</p>\",\"PeriodicalId\":20011,\"journal\":{\"name\":\"Pharmaceutical patent analyst\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2021-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"8\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical patent analyst\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4155/ppa-2020-0028\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2021/1/14 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical patent analyst","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4155/ppa-2020-0028","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2021/1/14 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 8

摘要

mRNA翻译的改变在确定细胞蛋白质组的变化中起着至关重要的作用。真核起始因子4E被丝裂原激活的蛋白激酶相互作用激酶(Mnks)磷酸化,导致特定致癌蛋白mrna的释放和翻译。近年来,制药行业开发新型化学骨架以制造有效和选择性的Mnk抑制剂的努力取得了丰硕成果。吡啶酮-动物支架已被用于生成多个系列的Mnk抑制剂,并在多个专利申请和研究文章中提出。Tomivosertib (eFT508)就是具有这种支架的分子之一。它是首批进入临床试验的两种Mnk抑制剂之一,并已显示出对几种实体和血液系统癌症的重大活性。本文通过对近5年来相关专利申请的分析,简要回顾了吡酮-氨基衍生的Mnk抑制剂的发展现状。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Mnk inhibitors: a patent review.

The alteration of mRNA translation has a crucial role in defining the changes in cellular proteome. The phosphorylation of eukaryotic initiation factor 4E by mitogen-activated protein kinase-interacting kinases (Mnks) leads to the release and translation of mRNAs of specific oncogenic proteins. In recent years, the efforts made by the pharmaceutical industry to develop novel chemical skeletons to create potent and selective Mnk inhibitors have been fruitful. The pyridone-aminal scaffold has been utilized to generate several series of Mnk inhibitors presented in multiple patent applications and research articles. Tomivosertib (eFT508) is one of the molecules with such scaffold. It is one of the first two Mnk inhibitors that entered clinical trials, and has displayed momentous activity against several solid and hematological cancers. The present compilation provides a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years.

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
Pharmaceutical patent analyst
Pharmaceutical patent analyst PHARMACOLOGY & PHARMACY-
CiteScore
1.80
自引率
0.00%
发文量
22
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信