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Description: Brefeldin A (also known as BFA), a fungal metabolite, is a potent macrocyclic lactone antibiotic and ATPase inhibitor for intracellular vesicle formation and protein transport (protein trafficking between the endoplasmic reticulum (ER) and the Golgi apparatus) with IC50 of 0.2 uM in HCT 116 cells. It has antitumor, antifungal, and antiviral effects. It induces cancer cell differentiation and apoptosis. Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release. BFA induced cells apoprosis (colorectal cancer cell line HCT116 ) by inhibiting ATP which functioned in the process of cellular vesicle trafficking.
References: Bioorg Med Chem. 2000 Feb; 8(2):455-63; Leuk Res. 2007 Dec; 31(12):1687-700.
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