Rationally Designed Amanitins Achieve Enhanced Cytotoxicity

Autor:	Mihajlo Todorovic, Paul Rivollier, Antonio A. W. L. Wong, Zhou Wang, Alla Pryyma, Tuan Trung Nguyen, Kayla C. Newell, Juliette Froelich, David M. Perrin
Rok vydání:	2022
Předmět:	Amanitins HEK293 Cells Liver Drug Discovery Molecular Medicine Humans Peptides HeLa Cells
Zdroj:	Journal of medicinal chemistry. 65(15)
ISSN:	1520-4804
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49543a0f84695a59e77bf9210066ab09 https://pubmed.ncbi.nlm.nih.gov/35696491 Zobrazit plný text záznamu