Brefeldin A
Protein trafficking inhibitor; Inhibits Sec7-containing guanine-exchange factor (GEF)
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Brefeldin A is a fungal lactone antibiotic, produced by many species, including Eupenicillium brefeldianum (Klausner et al.). It reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum by indirect inhibition of ADP-ribosylation factor (ARF; Klausner et al.; Helms & Rothman; Robinson et al.; Morinaga et al.; Moss & Vaughan; Nebenführ et al.; Ktistakis et al.). Brefeldin A binds to Sec7-containing guanine-exchange factor (GEF) at the ARF-GDP-Sec7 interface, preventing the conformational change required to release GDP and activate ARF (Mossessova et al.).
CELL LINE DEVELOPMENT
- Improves clustered regularly interspaced palindromic repeats (CRISPR)-mediated homology-directed repair (HDR) in mouse embryonic stem cells (Yu et al.).
CANCER RESEARCH
- Induces apoptosis in human leukemia (HL60, K562) and colon carcinoma (HT-29) cell lines (Shao et al.).
- Reduces survival, induces apoptosis and inhibits clonogenic activity of Colo 205 colorectal cancer stem cell line (Tseng et al.).