Inhibitors of the cellular trafficking of ricin.
Throughout the last decade, efforts to identify and develop effective inhibitors of the ricin toxin have focused on targeting its N-glycosidase activity. Alternatively, molecules disrupting intracellular trafficking have been shown to block ricin toxicity. Several research teams have recently developed high-throughput phenotypic screens for small molecules acting on the intracellular targets required for entry of ricin into cells. These screens have identified inhibitory compounds that can protect cells, and sometimes even animals against ricin. We review these newly discovered cellular inhibitors of ricin intoxication, discuss the advantages and drawbacks of chemical-genetics approaches, and address the issues to be resolved so that the therapeutic development of these small-molecule compounds can progress.
['Barbier|Julien|J|', 'Bouclier|Céline|C|', 'Johannes|Ludger|L|', 'Gillet|Daniel|D|']
D000818:Animals D001549:Benzamides D001570:Benzodiazepinones D004353:Drug Evaluation, Preclinical D057166:High-Throughput Screening Assays D006801:Humans D011485:Protein Binding D021381:Protein Transport D012276:Ricin D013876:Thiophenes
ricin chemical genetics retrograde transport small-molecule inhibitor