当前位置: X-MOL 学术J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Rationally Designed Amanitins Achieve Enhanced Cytotoxicity
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2022-06-13 , DOI: 10.1021/acs.jmedchem.1c02226
Mihajlo Todorovic 1 , Paul Rivollier 1 , Antonio A W L Wong 1 , Zhou Wang 1 , Alla Pryyma 1 , Tuan Trung Nguyen 1 , Kayla C Newell 1 , Juliette Froelich 1 , David M Perrin 1
Affiliation  

For 70 years, α-amanitin, the most cytotoxic peptide in its class, has been without a synthetic rival; through synthesis, we address the structure–activity relationships to inform the design of new amatoxins and disclose analogues that are more cytotoxic than the natural product when evaluated on CHO, HEK293, and HeLa cells, whereas on liver-derived HepG2 cells, the same toxins show diminished cytotoxicity.

中文翻译:

合理设计的鹅膏菌素实现增强的细胞毒性

70 年来,α-鹅膏菌素是同类中最具细胞毒性的肽,一直没有合成竞争对手。通过合成,我们解决了结构-活性关系,为新石蒜毒素的设计提供信息,并揭示了在 CHO、HEK293 和 HeLa 细胞上评估时比天然产物更具细胞毒性的类似物,而在肝源性 HepG2 细胞上,相同的毒素显示细胞毒性减弱。
更新日期:2022-06-13
down
wechat
bug