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

Abstract : 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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https://hal.inrae.fr/hal-03320788
Contributor : Camille Serva <>
Submitted on : Monday, August 16, 2021 - 2:13:25 PM
Last modification on : Wednesday, August 18, 2021 - 3:26:36 AM

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Hajer Abdelkafi, Aurélien Michau, Valérie Pons, Flora Ngadjeua, Alexandra Clerget, et al.. Structure–Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin. Journal of Medicinal Chemistry, American Chemical Society, 2020, 63 (15), pp.8114-8133. ⟨10.1021/acs.jmedchem.0c00298⟩. ⟨hal-03320788⟩

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