Antifolates: current developments.
In summary, the problem of MTX resistance has been approached in a mechanistic fashion, based on the wealth of information generated over the years. To date, these strategies have produced several new classes of anticancer drugs, with a variety of anticipated and unanticipated mechanisms of action. Several of these have shown promising preclinical activity, and these are moving into more stringent testing in the clinic.
Rayl
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Department of Internal Medicine, Yale University School of Medicine, New Haven, CT 06520-8032, USA.
Pizzorno
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D000630:Aminopterin / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000494:pharmacology*; D004351:Drug Resistance; D005493:Folic Acid Antagonists / Q000494:pharmacology*; D006801:Humans; D008727:Methotrexate / Q000493:pharmacokinetics / Q000494:pharmacology; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors
D000964:Antimetabolites, Antineoplastic; D005493:Folic Acid Antagonists; D013940:Thymidylate Synthase; C040210:edatrexate; D000630:Aminopterin; D008727:Methotrexate