Further, inhibition of FASN catalytic activity by agents such as cerulenin and C75 preferentially induce apoptosis of cancer cells (Pizer et al.
For example, cerulenin and C75 are commonly used as inhibitors of FASN through inhibition of the reaction of [beta]-ketoacyl synthase on FASN.
Cerulenin is the first FASN inhibitor identified and is a natural metabolic product used in antibiotics [33, 34, 61, 77].
In 2000, Lotfus and his fellow colleagues reported a small molecule, a structurally modified form of Cerulenin to be a novel FASN inhibitor, the C75 .
indicates that extracts of Fallopia multiflora can both reversibly and irreversibly inhibit FASN and exhibit a better inhibitory effect than both Cerulenin and C75 .
Consequently, increasing effort in therapeutics has focused on the development of drugs such as TOFA, C75, and cerulenin that target the fatty acid metabolic pathway to inhibit synthesis.
Since the ACC inhibitor TOFA decreases malonyl CoA while the two FASN inhibitors (C75, cerulenin) increase malonyl-CoA, it was anticipated that TOFA would enhance while C75 and cerulenin would inhibit CPT1A and fatty acid [beta]-oxidation [8, 11, 12].
FAS inhibitor cerulenin
reduces food intake and melanocortin receptor gene expression without modulating the other (an)orexigenic neuropeptides in chickens.
In the in vitro trial, T47D and MCF-7 cancer cells were cultured and then treated with canola oil and two common anti-cancer drugs: tamoxifen and cerulenin
. Measures used were cancer cell growth and activity of caspase-3 and p53 (proteins believed to promote cancer cell death and commonly used for assessing breast cancer treatment).
In an effort to thwart the above growing disparity, this research attempted to delineate the fundamental molecular differences between lean and steatotic livers through preconditioning with a fatty acid synthase inhibitor, Cerulenin
. Fatty acid synthase inhibition with Cerulenin
demonstrated a protective effect toward hepatic ischemia/reperfusion injury.
was the first characterized FASN inhibitor derived from the fungus Cephalosporum caerulens (Omura 1976).
is an antibiotic that is effective at inhibiting the passage of fatty acids from the cytoplasm to the mitochondria.