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Abdelkafi et al 17022020.pdf (1.34 MB)
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Structure-Activity Relationship Studies of Retro-1 Analogues Against Shiga Toxin

preprint
submitted on 17.02.2020 and posted on 20.02.2020 by Hajer Abdelkafi, Aurélien Michau, Valérie Pons, Flora Ngadjeua, Alexandra Clerget, Lilia Ait Ouarab, David-Alexandre Buisson, Lucie Caramelle, Daniel Gillet, Julien Barbier, Jean-Christophe Cintrat

The Retro-1 molecule was identified in a high-throughput screening as an inhibitor of ricin and Shiga toxins by diminishing their intracellular trafficking via the retrograde route, from early endosomes to the Golgi apparatus. In order to improve the activity of Retro-1, a SAR study was undertaken yielding an analog that possesses roughly 70-fold better EC50 against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.

Funding

Chemical genetics of the retrograde transport route – RETROscreen

Agence Nationale de la Recherche

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History

Email Address of Submitting Author

jean-christophe.cintrat@cea.fr

Institution

CEA

Country

France

ORCID For Submitting Author

0000-0001-5758-8077

Declaration of Conflict of Interest

no conflict of interest

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in Journal of Medicinal Chemistry

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