Brefeldin A

Brefeldin A (BFA) (IC50 value of 0.2 μM) is an inhibitor of ATPase.

ATPase is a chemical enzyme. It is essential in the ADP/ATP exchange providing chemical potential energy. ATP supplies the energy for such physiological activities such as importing metabolites necessary for cell metabolism, exporting toxins, wastes, and solutes that can hinder cellular processes, cell proliferation, ER stress and so forth.

When tested with cell line HEK293 cells (stably express wild-type (wt) CRELD2), BFA treatment nearly abolished the secretion of wtCRELD2 completely via inhibiting the transportation of proteins from the ER to the Golgi apparatus [4]. In MCF-7 cells and Hela cells, treatment with BFA induced p53 expression via inhibiting ATP which enhanced ER stress [5]. When treated with colorectal cancer cell line HCT116 cells, BFA treatment induced cells apoprosis by inhibiting ATP which functioned in the process of cellular vesicle trafficking

Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release.

BFA also is reported as an inhibitor for GTP/GDP exchange in a dose-dependent way, which is important in vesicular trafficking.