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The cancer stem cell selective inhibitor salinomycin is a p-glycoprotein inhibitor.
- Source :
-
Blood cells, molecules & diseases [Blood Cells Mol Dis] 2010 Jun 15; Vol. 45 (1), pp. 86-92. Date of Electronic Publication: 2010 May 04. - Publication Year :
- 2010
-
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.<br /> (Copyright 2010 Elsevier Inc. All rights reserved.)
- Subjects :
- ATP Binding Cassette Transporter, Subfamily B, Member 1 genetics
Apoptosis drug effects
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Humans
Up-Regulation
ATP Binding Cassette Transporter, Subfamily B, Member 1 antagonists & inhibitors
ATP Binding Cassette Transporter, Subfamily B, Member 1 metabolism
Anti-Bacterial Agents pharmacology
Drug Resistance, Neoplasm drug effects
Neoplasms drug therapy
Neoplastic Stem Cells drug effects
Pyrans pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1096-0961
- Volume :
- 45
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Blood cells, molecules & diseases
- Publication Type :
- Academic Journal
- Accession number :
- 20444629
- Full Text :
- https://doi.org/10.1016/j.bcmd.2010.03.008