Identification of novel inhibitors of UDP-Glc 4′-epimerase, a validated drug target for african sleeping sickness

Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4′-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells.

Graphical abstractNovel inhibitors of Trypanosoma brucei and human UDP-Glc 4′-epimerase with micromolar potency were identified by screening marine natural products and drug-like molecules.Figure optionsDownload full-size imageDownload as PowerPoint slide