The antifolates.

Michele Visentin, Rongbao Zhao, I David Goldman

Hematology/oncology clinics of North America 2012 Jun

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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.