Antifolate Drugs in Cancer Therapy

1 Antifolate Drugs: Past and Future Perspectives.- 2 Folate Biochemistry in Relation to Antifolate Selectivity.- 3 Clinical Pharmacology and Resistance to Dihydrofolate Reductase Inhibitors.- 4 Development of Nonpolyglutamatable DHFR Inhibitors.- 5 Fluoropyrimidines as Antifolate Drugs.- 6 Raltitrexed (Tomudextm), a Highly Polyglutamatable Antifolate Thymidylate Synthase Inhibitor: Design and Preclinical Activity.- 7 Tomudex: Clinical Development.- 8 Preclinical Pharmacology Studies and the Clinical Development of a Novel Multitargeted Antifolate, MTA (LY231514).- 9 GW1843: A Potent, Noncompetitive Thymidylate Synthase Inhibitor—Preclinical and Preliminary Clinical Studies.- 10 Preclinical and Clinical Studies with the Novel Thymidylate Synthase Inhibitor Nolatrexed Dihydrochloride (Thymitaqtm, AG337).- 11 ZD9331: Preclinical and Clinical Studies.- 12 Preclinical and Clinical Evaluation of the Glycinamide Ribonucleotide Formyltransferase Inhibitors Lometrexol and LY309887.- 13 AG2034: A GARFT Inhibitor with Selective Cytotoxicity to Cells that Lack a G1 Checkpoint.- 14 Receptor- and Carrier-Mediated Transport Systems for Folates and Antifolates: Exploitation for Folate-Based Chemotherapy and Immunotherapy.- 15 Folates as Chemotherapeutic Modulators.- 16 Antifolate Polyglutamylation in Preclinical and Clinical Antifolate Resistance.- 17 Antifolates in Combination Therapy.- 18 Pharmacodynamic Measurements and Predictors of Response to Thymidylate Synthase Inhibitors.- 19 Molecular Regulation of Expression of Thymidylate Synthase.- 20 The Role of Uracil Misincorporation in Thymineless Death.- 21 Thymineless Death.- 22 Genetic Determinants of Cell Death and Toxicity.