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• W2022209987 abstract "Cruentaren A, a new antifungal benzolactone produced by the myxobacterium Byssovorax cruenta, proved to be highly cytotoxic against various human cell lines. It inhibited the proliferation of different cancer cell lines including a multidrug-resistant KB line at low nanomolar levels. It arrested human histocytic lymphoma cells (U-937) in G(0/1) phase, but did not trigger an apoptotic process. Studies to uncover the molecular target of cruentaren A showed that the novel compound, despite its structural similarity to the benzolactone enamides apicularen and salicylihalamide, was no V-ATPase inhibitor. In contrast, cruentaren specifically inhibited mitochondrial F(O)F(1)-ATPases with IC50 values of 15-30 nM. Although the exact binding site of cruentaren remains undefined, inhibition was shown to occur by interaction with the catalytic F(1) domain. Since mitochondrial ATPases play a crucial role in the pathophysiology of several human disorders including cancer, cruentaren or synthetic derivatives thereof could form the basis of future therapeutic strategies." @default.
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• W2022209987 date "2007-07-03" @default.
• W2022209987 modified "2023-10-13" @default.
• W2022209987 title "Cruentaren A, a highly cytotoxic benzolactone from<i>Myxobacteria</i>is a novel selective inhibitor of mitochondrial F₁-ATPases" @default.
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• W2022209987 doi "https://doi.org/10.1016/j.febslet.2007.06.069" @default.
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