Description
Brefeldin A is a lactone antibiotic found in fungi such as Eupenicillium; it exhibits anticancer and antiviral activities. Brefeldin A inhibits activity of guanine nucleotide exchange factors, preventing association with COPI and COPI-mediated vesicle formation and suppressing protein transport from the endoplasmic reticulum to the Golgi apparatus. Brefeldin A is used in research models to study endoplasmic reticulum stress and protein transport. In vitro, this compound inhibits poliovirus replication. In prostate cancer cells, brefeldin A inhibits cell growth, induces apoptosis and G1 phase cell cycle arrest, decreases levels of p53, CDK2, CDK4, and cyclin D1, and causes cell death.
References
Zhou C, Li C, Li D, et al. BIG1, a brefeldin A-inhibited guanine nucleotide-exchange protein regulates neurite development via PI3K-AKT and ERK signaling pathways. Neuroscience. 2013 Dec 19;254:361-8. PMID: 24090963.
Rouhana J, Padilla A, Estaran S, et al. Kinetics of interaction between ADP-ribosylation factor-1 (Arf1) and the Sec7 domain of Arno guanine nucleotide exchange factor, modulation by allosteric factors, and the uncompetitive inhibitor brefeldin A. J Biol Chem. 2013 Feb 15;288(7):4659-72. PMID: 23255605.
Chapman JR, Tazaki H, Mallouh C, et al. Brefeldin A-induced apoptosis in prostatic cancer DU-145 cells: a possible p53-independent death pathway. BJU Int. 1999 Apr;83(6):703-8. PMID: 10233583.
Cuconati A, Molla A, Wimmer E. Brefeldin A inhibits cell-free, de novo synthesis of poliovirus. J Virol. 1998 Aug;72(8):6456-64. PMID: 9658088.
