Abstract
Expression of the multidrug resistance (MDR) phenotype is responsible for chemotherapy failure in numerous cancers. Overexpression of mdr1 gene-encoded permeability glycoprotein (P-gp) is known to play a pivotal role in the development of this phenotype. The role of P-gp has been proposed as an important goal in the design of chemotherapy strategies. However, modulation of P-gp activity by chemotherapy has limited possibilities because of toxicity and poor specificity. In this article, we review the latest advancements in different potential P-gp-mediated MDR reversal mechanisms as well as the methods of evaluating MDR reversal activity, which would be helpful in finding novel MDR reversal agents (or chemosensitizers).
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / biosynthesis*
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology
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Apoptosis / physiology
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Drug Resistance, Multiple / genetics
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Drug Resistance, Multiple / immunology
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Drug Resistance, Multiple / physiology*
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Drug Resistance, Neoplasm / genetics
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Drug Resistance, Neoplasm / immunology
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Drug Resistance, Neoplasm / physiology*
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Genes, MDR
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Humans
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents