期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 15, 页码 8114-8133出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00298
关键词
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资金
- French National Agency for Research (ANR) [ANR-11BSV2-0018]
- joint ministerial program of R&D against CBRNe risks
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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