Rationally Designed Amanitins Achieve Enhanced Cytotoxicity.

ID: ALA5113439

Journal: J Med Chem

Title: Rationally Designed Amanitins Achieve Enhanced Cytotoxicity.

Authors: Todorovic M, Rivollier P, Wong AAWL, Wang Z, Pryyma A, Nguyen TT, Newell KC, Froelich J, Perrin DM.

Abstract: 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.

CiteXplore: 35696491

DOI: 10.1021/acs.jmedchem.1c02226

Patent ID: ┄