The cancer stem cell selective inhibitor salinomycin is a p-glycoprotein inhibitor.

Article Details

Citation

Copy to clipboard

Riccioni R, Dupuis ML, Bernabei M, Petrucci E, Pasquini L, Mariani G, Cianfriglia M, Testa U

The cancer stem cell selective inhibitor salinomycin is a p-glycoprotein inhibitor.

Blood Cells Mol Dis. 2010 Jun 15;45(1):86-92. doi: 10.1016/j.bcmd.2010.03.008. Epub 2010 May 4.

PubMed ID

20444629 [ View in PubMed

]

Abstract

Salinomycin, a polyether antibiotic acting as a highly selective potassium ionophore and widely used as an anticoccidial drug, was recently shown to act as a specific inhibitor of cancer stem cells. In the present study we report that salinomycin acts as a potent inhibitor of multidrug resistance gp170, as evidenced through drug efflux assays in MDR cancer cell lines overexpressing P-gp (CEM-VBL 10 and CEM-VBL 100; A2780/ADR). Conformational P-gp assay provided evidence that the inhibitory effect of salinomycin on P-gp function could be mediated by the induction of a conformational change of the ATP transporter. Treatment of the MDR cell lines with salinomycin restored a normal drug sensitivity of these cells. The observation that salinomycin is a MDR-1 inhibitor may have important implications for the understanding of the mechanisms through which this drug impairs the viability of cancer stem cells. Interestingly, nigericin and abamectin, two additional drugs identified as cancer stem cells inhibitors, also act as potent gp170 inhibitors.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Salinomycin	P-glycoprotein 1	Protein	Humans	Unknown	Inhibitor	Details