Innentitelbild: Development of a FUT8 Inhibitor with Cellular Inhibitory Properties (Angew. Chem. 52/2024)

Dr. Yoshiyuki Manabe, Dr. Tomoyuki Takebe, Satomi Kasahara, Koki Hizume, Dr. Kazuya Kabayama, Prof. Yoshihiro Kamada, Akiko Asakura, Prof. Shinichiro Shinzaki, Dr. Shinji Takamatsu, Prof. Eiji Miyoshi, Ana García-García, Dr. Sergey Y. Vakhrushev, Prof. Ramón Hurtado-Guerrero, Prof. Koichi Fukase
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Abstract

Core fucosylation, catalyzed by α-1,6-fucosyltransferase (FUT8), is implicated in various diseases, making FUT8 inhibitors highly desirable. In their Research Article (e202414682), Yoshiyuki Manabe, Koichi Fukase et al. developed FUT8 inhibitors with potent cellular activity. Through high-throughput screening and structural optimization, potent FUT8 inhibitors were identified. Additionally, prodrug derivatization enhanced the stability of these inhibitors, enabling the suppression of core fucose expression in cell-based assays.

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一种具有细胞抑制特性的FUT8抑制剂的研制化学52/2024)
由α-1,6-聚焦转移酶(FUT8)催化的核心聚焦化与多种疾病有关,因此非常需要FUT8抑制剂。在他们的研究文章(e202414682)中,Yoshiyuki Manabe, Koichi Fukase等人。开发出具有强大细胞活性的FUT8抑制剂。通过高通量筛选和结构优化,确定了有效的FUT8抑制剂。此外,前药衍生化增强了这些抑制剂的稳定性,从而能够在基于细胞的检测中抑制核心病灶的表达。
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来源期刊
Angewandte Chemie
Angewandte Chemie 化学科学, 有机化学, 有机合成
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