Squalene epoxidase catalyzes the first oxygenation step in sterol biosynthesis and is thought to be one of the rate-limiting enzymes in this pathway. In constrast, inhibition of rat liver squalene epoxidase only occurs at higher drug concentrations (K i =77 μ m), and is competitive with squalene. NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. This inhibition of enzyme activity results in decreased amounts of sterols, especially ergosterol, and a corresponding accumulation of squalene in the cells. Squalene monooxygenase (also called squalene epoxidase) is an enzyme that uses NADPH and molecular oxygen to oxidize squalene to 2,3-oxidosqualene (squalene epoxide). Start studying Antifungal Drugs. In humans, squalene epoxidase is encoded by the SQLE gene. Terbinafine SF 86-327 is one of the allylamines, which were developed as synthetic antifungal drugs (22). In Vitro NB-598 (10 μM) causes a 36±7% reduction in total cholesterol level of MIN6 cells. Specific inhibitors of squalene epoxidase such as terbinafine have been reported. Thus, terbinafine has no effect on cholesterol biosynthesis in vivo. squalene epoxidase inhibitors, diacyl glycerol acyl transferase inhibitors, ATP citrate ly ase inhibitors have shown a promising potential in the treatment of hyperlipidemia in clinical trials. Specific inhibitors of squalene epoxidase such as terbinafine have been reported. In eukaryotes, squalene is oxidized by squalene epoxidase and then enzymatically cyclized in the first step of steroid biosynthesis. Horie M(1), Iwasawa Y, Satoh T, Shimizu A, Nagata Y, Kamei T. Author information: (1)Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan. Search. Liranaftate can be used for the research of dermatophytes. Terbinafine has ] The squalene epoxidase inhibitor containing the compound represented by these or its pharmaceutically acceptable salt as an active ingredient. Effects of NB-598, a potent squalene epoxidase inhibitor, on the apical membrane uptake of cholesterol and basolateral membrane secretion of lipids in Caco-2 cells. Terbinafine has been studied in detail and has been shown to perform its antifungal activity by inhibiting squalene epoxidase … Although the exact mechanism of action against fungi is not known, naftifine appears to interfere with sterol biosynthesis by inhibiting the enzyme squalene 2,3-epoxidase. Terbinafine is a potent non‐competitive inhibitor of squalene epoxidase from Candida (K i =30n m). Liranaftate (Piritetrate) is a squalene epoxidase inhibitor with anti-fungicidal activities. Liranaftate also suppresses fungal element-promoted production of IL-8 and experimental inflammation. 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