Drug intelligence / Profile preview

cerulenin

Development stage
Unknown
Modality
Small Molecules
01

Overview

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.

Other names
Helicocerin3-Nona‑4,7‑dienoyl‑oxirane‑2-carboxylic acid amide(2R,3S)-3‑[(4E,7E)-Nona‑4,7-dienoyl]oxirane‑2-carboxamide
02

Targets

Fatty acid synthase beta-ketoacyl-ACP synthase domainHMGCS1 (3-hydroxy-3-methylglutaryl-CoA synthase 2 (mitochondrial))

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