Journal of Medicinal Chemistry p. 8114 - 8133 (2020)
Update date:2022-08-15
Topics:
Abdelkafi, Hajer
Michau, Aurélien
Pons, Valérie
Ngadjeua, Flora
Clerget, Alexandra
Ait Ouarab, Lilia
Buisson, David-Alexandre
Montoir, David
Caramelle, Lucie
Gillet, Daniel
Barbier, Julien
Cintrat, Jean-Christophe
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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