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Cerulenin
- indication:For use as a biochemical tool, Cerulenin is shown to cause dramatic weight loss in animals
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Oral, mouse LD<sub>50</sub>: 547 mg/kg. Symptoms of overexposure include moderate to severe erythema (redness) and moderate edema (raised skin), nausea, vomiting, and headache.
- absorprion:
- halflife:
- roouteelimination:
- volumedistribution:
- clearance: