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

Journal of Medicinal Chemistry
2020.0

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 (EC<sub>50</sub>) against Shiga toxin cytotoxicity measured in a cell protein synthesis assay.

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