Mechanism action of Cerulenin
Irreversibly binds to fatty acid synthase, specifically b-ketoacyl-acyl
carrier protein synthase (FabH, FabB and FabF condensation enzymes). A
number of tumor cells and cell lines have been observed to have highly
upregulated expression and activity of fatty acid synthase (FAS).
Inhibition of FAS by cerulenin leads to cytotoxicity and apoptosis in
human cancer cell lines, an effect believed to be mediated by the
accumulation of malonyl-coenzyme A in cells with an upregulated FAS
pathway.
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