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A new class of ribosomally synthesized and post-translationally modified peptides (RiPPs), named asperigimycins, was isolated from the toxic fungus Aspergillus flavus and shown to have potent, selective activity against leukemia cells. Lipid modification enhanced cell entry via the SLC46A3 gene. Asperigimycins disrupt cell division and represent a promising direction for anti-cancer drug development.