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

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...

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Veröffentlicht in:Angewandte Chemie 2024-12, Vol.136 (52), p.n/a
Hauptverfasser: Manabe, Yoshiyuki, Takebe, Tomoyuki, Kasahara, Satomi, Hizume, Koki, Kabayama, Kazuya, Kamada, Yoshihiro, Asakura, Akiko, Shinzaki, Shinichiro, Takamatsu, Shinji, Miyoshi, Eiji, García‐García, Ana, Vakhrushev, Sergey Y., Hurtado‐Guerrero, Ramón, Fukase, Koichi
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container_issue 52
container_start_page
container_title Angewandte Chemie
container_volume 136
creator Manabe, Yoshiyuki
Takebe, Tomoyuki
Kasahara, Satomi
Hizume, Koki
Kabayama, Kazuya
Kamada, Yoshihiro
Asakura, Akiko
Shinzaki, Shinichiro
Takamatsu, Shinji
Miyoshi, Eiji
García‐García, Ana
Vakhrushev, Sergey Y.
Hurtado‐Guerrero, Ramón
Fukase, Koichi
description 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.
doi_str_mv 10.1002/ange.202420450
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title Innentitelbild: Development of a FUT8 Inhibitor with Cellular Inhibitory Properties (Angew. Chem. 52/2024)
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