研究动态
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针对F-BOX蛋白的抑制剂。

Inhibitors Targeting the F-BOX Proteins.

发表日期:2023 Aug 25
作者: Yalnaz Naseem, Chaofeng Zhang, Xinyi Zhou, Jianshu Dong, Jiachong Xie, Huimin Zhang, Clement Agboyibor, YueFeng Bi, Hongmin Liu
来源: Protein & Cell

摘要:

F-box蛋白通过泛素化和随后的靶标废弃来参与多个细胞过程。F-box蛋白介导的蛋白质降解中的任何重要突变都可能导致人类畸形。F-box蛋白参与的各种细胞过程包括细胞增殖、凋亡、侵袭、血管生成和转移。为了靶向F-box蛋白及其相关信号通路进行癌症治疗,研究人员已经开发了数千种F-box抑制剂。最先进的FBW7抑制剂NVD-BK M120是一种强效的P13激酶抑制剂,已经被证实可以通过破坏被称为MCL1的蛋白质的水平,在癌性人肺细胞中引发凋亡。此外,F-box抑制剂已经通过靶向特定突变蛋白质在治疗某些癌症方面展示出了其疗效。本文研究了F-box蛋白的作用方式以及其对恶性发展的贡献,从而深入了解靶向F-box蛋白及其信号通路的抑制剂,最终确定了最有前景的抗癌治疗方法。© 2023. 该作者(们),在Springer Science+Business Media, LLC,Springer Nature的独家许可下。
F-box proteins are involved in multiple cellular processes through ubiquitylation and consequent degradation of targeted substrates. Any significant mutation in F-box protein-mediated proteolysis can cause human malformations. The various cellular processes F-box proteins involved include cell proliferation, apoptosis, invasion, angiogenesis, and metastasis. To target F-box proteins and their associated signaling pathways for cancer treatment, researchers have developed thousands of F-box inhibitors. The most advanced inhibitor of FBW7, NVD-BK M120, is a powerful P13 kinase inhibitor that has been proven to bring about apoptosis in cancerous human lung cells by disrupting levels of the protein known as MCL1. Moreover, F-box Inhibitors have demonstrated their efficacy for treating certain cancers through targeting particular mutated proteins. This paper explores the key studies on how F-box proteins act and their contribution to malignancy development, which fabricates an in-depth perception of inhibitors targeting the F-box proteins and their signaling pathways that eventually isolate the most promising approach to anti-cancer treatments.© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.