ABCG2: the key to chemoresistance in cancer stem cells?
Article Details
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An Y, Ongkeko WM
ABCG2: the key to chemoresistance in cancer stem cells?
Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1529-42. doi: 10.1517/17425250903228834.
- PubMed ID
- 19708828 [ View in PubMed]
- Abstract
Multi-drug chemoresistance remains one of the most common reasons for chemotherapy failure. The membrane transporter protein ABCG2/BCRP1 has been shown in vitro to effectively reduce the intracellular concentrations of several prominent anticancer chemotherapeutic agents such as mitoxantrone and doxorubicin. Intriguingly, cancer stem cells are known to be characterized by multi-drug chemoresistance. Taking into account that the ABCG2(+) subset of tumor cells are often enriched with cells with cancer stem-like phenotypes, it has been proposed that ABCG2 activity underlies the ability of cancer cells to regenerate post-chemotherapy. Furthermore, we also review evidence suggesting that tyrosine kinase inhibitors, including imatinib and gefitinib, are both direct and downstream inactivators of ABCG2 and, therefore, serve as candidates to reverse cancer stem cell chemoresistance and potentially target cancer stem cells.
DrugBank Data that Cites this Article
- Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Doxorubicin ATP-binding cassette sub-family G member 2 Protein Humans UnknownSubstrateDetails Gefitinib ATP-binding cassette sub-family G member 2 Protein Humans UnknownSubstrateInhibitorDetails Imatinib ATP-binding cassette sub-family G member 2 Protein Humans NoSubstrateInhibitorDetails Mitoxantrone ATP-binding cassette sub-family G member 2 Protein Humans UnknownSubstrateDetails