Abstract
Multidrug resistance mediated by the overexpression of ABC transporters is a major challenge in cancer chemotherapy. Here, we report the synthesis of an organoruthenium complex, RuF, that was designed to surmount multidrug resistance by combining ABCG2 inhibition and cancer cell cytotoxicity, yielding synergistic efficacy.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily G, Member 2 / antagonists & inhibitors*
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ATP Binding Cassette Transporter, Subfamily G, Member 2 / genetics
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ATP Binding Cassette Transporter, Subfamily G, Member 2 / metabolism
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Cycle / drug effects
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Resistance, Multiple / drug effects*
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Drug Resistance, Neoplasm / drug effects*
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Drug Screening Assays, Antitumor
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Humans
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Molecular Structure
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Neoplasm Proteins / antagonists & inhibitors*
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Neoplasm Proteins / genetics
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Neoplasm Proteins / metabolism
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Organometallic Compounds / chemistry
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Organometallic Compounds / pharmacology*
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Ruthenium / chemistry
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Ruthenium / pharmacology*
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Structure-Activity Relationship
Substances
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ABCG2 protein, human
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ATP Binding Cassette Transporter, Subfamily G, Member 2
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Antineoplastic Agents
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Neoplasm Proteins
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Organometallic Compounds
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Ruthenium