Apoptolidin, originally isolated from a Nocardiopsis sp., induces apoptotic cell death in rat glial cells transformed with the adenovirus E1A oncogene (IC50 = 11 ng/ml). Apoptolidin is among the most selective cytotoxic agents tested by the NCI in human cancer cell lines. Although the apoptotic activity of apoptolidin correlates with F0F1-ATPase inhibition, recent evidence suggests the existence of a secondary biological target or more complex mode of action.
1) Kim et al. (1997), Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp.; J. Antibiot. (Tokyo), 50 628
2) Salomon et al. (2001), Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase; Chem. Biol., 8 71
3) Wender et al. (2006), Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues; Org. Lett., 8 589
