一种具有细胞抑制特性的FUT8抑制剂的研制化学52/2024)

Angewandte Chemie Pub Date : 2024-11-02 DOI:10.1002/ange.202420450

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

{"title":"一种具有细胞抑制特性的FUT8抑制剂的研制化学52/2024)","authors":"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","doi":"10.1002/ange.202420450","DOIUrl":null,"url":null,"abstract":"<p><b>Core fucosylation</b>, 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.\n <figure>\n <div><picture>\n <source></source></picture><p></p>\n </div>\n </figure>\n </p>","PeriodicalId":7803,"journal":{"name":"Angewandte Chemie","volume":"136 52","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ange.202420450","citationCount":"0","resultStr":"{\"title\":\"Innentitelbild: Development of a FUT8 Inhibitor with Cellular Inhibitory Properties (Angew. Chem. 52/2024)\",\"authors\":\"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\",\"doi\":\"10.1002/ange.202420450\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><b>Core fucosylation</b>, 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.\\n <figure>\\n <div><picture>\\n <source></source></picture><p></p>\\n </div>\\n </figure>\\n </p>\",\"PeriodicalId\":7803,\"journal\":{\"name\":\"Angewandte Chemie\",\"volume\":\"136 52\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-11-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ange.202420450\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Angewandte Chemie\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/ange.202420450\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Angewandte Chemie","FirstCategoryId":"1085","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/ange.202420450","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}

引用次数: 0

摘要

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。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

摘要图片

查看原文

微信好友朋友圈 QQ好友复制链接

本刊更多论文

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 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.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Angewandte Chemie 化学科学, 有机化学, 有机合成

自引率

0.00%

发文量

审稿时长

1 months