Abstract
This article focuses on the cellular, biochemical, and molecular pharmacology of antifolates and how a basic understanding of the mechanism of action of methotrexate, its cytotoxic determinants, mechanisms of resistance, and transport into and out of cells has led to the development of a new generation of antifolates, a process that continues in the laboratory and in the clinics. New approaches to folate-based cancer chemotherapy are described based on the targeted delivery of drugs to malignant cells.
Copyright © 2012 Elsevier Inc. All rights reserved.
MeSH terms
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Animals
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Antimetabolites, Antineoplastic / chemistry
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Antimetabolites, Antineoplastic / pharmacology
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Antimetabolites, Antineoplastic / therapeutic use
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Drug Resistance, Neoplasm
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Folic Acid / biosynthesis
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Folic Acid Antagonists / chemistry*
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Folic Acid Antagonists / pharmacology*
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Folic Acid Antagonists / therapeutic use
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Humans
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Methotrexate / chemistry
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Methotrexate / pharmacology
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Methotrexate / therapeutic use
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Molecular Targeted Therapy
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Neoplasms / drug therapy*
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Neoplasms / metabolism
Substances
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Antimetabolites, Antineoplastic
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Folic Acid Antagonists
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Folic Acid
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Methotrexate