Salinomycin is an antibacterial and coccidiostat ionophore therapeutic drug.
The mechanism of action by which salinomycin kills cancer stem cells involves lysosomal iron sequestration, leading to the production of reactive oxygen species, lysosome membrane permeabilization and ferroptosis. Studies performed in 2011 showed that salinomycin could induce apoptosis of human cancer cells at higher concentrations. C20 amino derivatives such as ironomycin have shown to be more potent in vitro models of persister cells cancer cells and in vivo . Promising results from a few clinical pilot studies reveal that salinomycin is able to effectively eliminate cancer stem cells and to induce partial clinical regression of heavily pretreated and therapy-resistant cancers. The ability of salinomycin to kill both cancer stem cells and therapy-resistant cancer cells (persister) may define the compound as a novel and an effective anticancer drug.C. Naujokat, R. Steinhart "Salinomycin as a Drug for Targeting Human Cancer Stem Cells”, Journal of Biomedicine and Biotechnology, Volume 2012 (2012), Article ID 950658, , open access review articleA. Huczyński, ”Polyether ionophores—promising bioactive molecules for cancer therapy”, Bioorganic & Medicinal Chemistry Letters, 2012,22, 7002-7010,, open access review article It has been also shown that salinomycin and its derivatives exhibit potent antiproliferative activity against the drug-resistant cancer cell lines.A. Huczyński, J. Janczak, M. Antoszczak, J. Wietrzyk, E. Maj, B. Brzezinski, ” Antiproliferative activity of salinomycin and its derivatives”, Bioorganic & Medicinal Chemistry Letters, 2012, 22, 7146-7150,, review article Salinomycin is the key compound in the pharmaceutical company Verastem's efforts to produce an anti-cancer-stem-cell drug.
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