Apoptolidin
Application Notes
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.
References
- Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues. Wender P.A. et al., Org. Lett. 2006, 8, 589.
- Apoptolidin: induction of apoptosis by a natural product. Daniel P.T. et al., Angew. Chem. Int. Ed. Engl. 2006, 45, 872.
- Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F(0)F(1)-ATPase. Salomon A.R. et al., Proc. Natl Acad. Sci. USA 2000, 97, 14766.