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Structure–Activity Relationship Studies of Retro‑1 Analogues against Shiga Toxin

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posted on 2020-07-27, 11:39 authored by Hajer Abdelkafi, Aurélien Michau, Valérie Pons, Flora Ngadjeua, Alexandra Clerget, Lilia Ait Ouarab, David-Alexandre Buisson, David Montoir, Lucie Caramelle, Daniel Gillet, Julien Barbier, Jean-Christophe Cintrat
High-throughput screening has shown that Retro-1 inhibits ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. To improve the activity of Retro-1, a structure–activity relationship (SAR) study was undertaken and yielded an analogue with a roughly 70-fold better half-maximal effective concentration (EC50) against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.

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