一项对基因激活蛋白激酶与相互作用激酶 (MNKs) 调制剂的专利审查 (2019年至今)
Qiang Li1,2, Xiang Chen2,3, Mingzhi Su2
1School of Pharmaceutical Sciences & Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, China.
Expert opinion on therapeutic patents
|December 21, 2024
概括
中原激活蛋白激酶相互作用激酶 (MNKs) 是癌症治疗的关键标. 最近的专利审查显示,强效和选择性的MNK抑制剂具有有希望的临床前结果,包括新的作用机制.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 药物发现 药物发现 药物发现
背景情况:
- 线素激活蛋白激酶相互作用激酶 (MNKs) 通过真核细胞启动因子4E (eIF4E) 酸化来调节蛋白转化.
- MNKs在瘤发生过程中发挥着关键作用,并与炎症,肥胖和癌症有关.
- 开发强效和选择性的MNK抑制剂是由于其治疗潜力的重大研究重点.
研究的目的:
- 审查2019年至2024年在专利中报告的MNK抑制剂.
- 提供可用的MNK抑制剂的景观,包括化学结构,活性和发育阶段.
主要方法:
- 在世界知识产权组织和欧洲专利局数据库中的专利文献搜索 (2019-2024年).
- 对报告的MNK抑制剂的分析,重点关注化学结构,生物活性和临床前/临床发展状态.
主要成果:
- 发现了高度强效和选择性的MNK抑制剂,具有有希望的临床前癌症模型结果.
- 识别新型抑制器骨架和机制,包括非传统的ATP竞争和化向的嵌合体.
- 大多数近期的小分子抑制剂与已知化合物如eFT508和ETC-206具有结构相似之处.
结论:
- 在最近的专利中报告了MNK抑制剂开发的重大进展.
- 新化合物在临床前癌症模型中显示出有效性,并探索新的治疗策略.
- 预计进一步的研究和临床试验将阐明MNK抑制剂的全部潜力,并揭示新的MNK功能.
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