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Cerulenin is a natural antifungal antibiotic isolated from the fungus Cephalosporium caerulens. It is primarily used as a biochemical tool in research rather than as an approved pharmaceutical agent. Cerulenin acts by irreversibly inhibiting fatty acid synthase (FAS), specifically binding to β-ketoacyl-acyl carrier protein synthase enzymes involved in fatty acid biosynthesis. This inhibition blocks the formation of new fatty acids and sterols in fungi and other organisms[1][3][4]. Cerulenin also inhibits HMG-CoA synthetase activity, affecting sterol synthesis pathways[1][5]. In addition to its antifungal properties, cerulenin has been shown to induce apoptosis and cytotoxicity in certain tumor cell lines due to its effects on lipid metabolism[1][3]. It can cause dramatic weight loss in animal models by mechanisms that are independent of leptin signaling but may involve increased energy availability sensed by AMPK in the hypothalamus[1][3]. Cerulenin is not approved for clinical use but is widely used as a research reagent.
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