期刊
PHARMACEUTICAL PATENT ANALYST
卷 10, 期 1, 页码 -出版社
FUTURE SCI LTD
DOI: 10.4155/ppa-2020-0028
关键词
inhibitor; kinases and patent; Mnk1 and Mnk2; tomivosertib
资金
- Australia Government National Health and Medical Research Council [1050825]
- South Australian Health and Medical Research Institute (Beat Cancer Project Principal Cancer Research Fellowship)
- Australian Government Research Training Program Scholarship
The alteration of mRNA translation plays a crucial role in defining cellular proteome changes, with efforts in developing novel Mnk inhibitors yielding successful results in the pharmaceutical industry. The pyridone-aminal scaffold, including molecules like Tomivosertib (eFT508), has shown significant activity against various cancers.
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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据