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

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