Lonidamine is an indazole compound that has been reported to inhibit angiogenic-related endothelial cell functions. This compound has been found to trigger apoptosis in endothelial cells and cause a decrease in proliferation, migration, invasion, and morphogenesis. The apoptotic effects of Lonidamine have been demonstrated to be due to Bax, Bid, caspase-3, and caspase-9 activation, as well as cytochrome c release. Futher studies show that Lonidamine prevents cellular energy metabolism via HXK (hexokinase) inhibition. This compound also blocks CFTR Cl- channels in vitro.
1. De Martino, C., et al. 1984. Oncology. 41: 15-29. PMID: 6717891
2. Gong, X., et al. 2002. Br. J. Pharmacol. 137: 928-936. PMID: 12411425
3. Del Bufalo, D., et al. 2004. Neoplasia. 6: 513-522. PMID: 15548359
4. Sánchez, Y., et al. 2010. J. Pharmacol. Exp. Ther. 335: 114-123. PMID: 20605902
See how others have used Lonidamine (CAS 50264-69-2). Click on the entry to view the PubMed entry .
PMID: 30151646 | Optical Redox Imaging of Lonidamine Treatment Response of Melanoma Cells and Xenografts. | Xu, HN. et al. 2019. Mol Imaging Biol. 21: 426-435.
PMID: 26521302 | Inhibition of Mitochondrial Complex II by the Anticancer Agent Lonidamine. | Guo, L. et al. 2016. J Biol Chem. 291: 42-57.
PMID: 25504852 | Lonidamine induces intracellular tumor acidification and ATP depletion in breast, prostate and ovarian cancer xenografts and potentiates response to doxorubicin. | Nath, K. et al. 2015. NMR Biomed. 28: 281-90.
PMID: 25702942 | Effects of hyperglycemia on lonidamine-induced acidification and de-energization of human melanoma xenografts and sensitization to melphalan. | Nath, K. et al. 2015. NMR Biomed. 28: 395-403.
PMID: 22745015 | (31) P and (1) H MRS of DB-1 melanoma xenografts: lonidamine selectively decreases tumor intracellular pH and energy status and sensitizes tumors to melphalan. | Nath, K. et al. 2013. NMR Biomed. 26: 98-105.
PMID: 24022342 | MiR-199a suppresses the hypoxia-induced proliferation of non-small cell lung cancer cells through targeting HIF1α. | Ding, G. et al. 2013. Mol Cell Biochem. 384: 173-80.