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Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity.
This folate antagonist structure-activity relationship can be of value for predicting drug sensitivity and resistance of tumor cells or drug-related toxicity to normal cells and for the rational design and development of novel antifolates.
Folate-based thymidylate synthase inhibitors as anticancer drugs.
  • A. Jackman, A. Calvert
  • Biology, Chemistry
    Annals of oncology : official journal of the…
  • 1 November 1995
A portfolio of novel compounds comprehensively addresses the potential of thymidylate synthase as a target for cancer chemotherapy.
bcl-2 modulation of apoptosis induced by anticancer drugs: resistance to thymidylate stress is independent of classical resistance pathways.
Resistance to thymidylate stress in bcl-2-expressing cells therefore occurred by a mechanism different from those which classically define resistance to this type of cytotoxic drug.
BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.
The data suggest that BGC 945 selectively inhibits thymidylate synthase in alpha-FR-overexpressing tumors and should cause minimal toxicity to humans at therapeutic doses.
Comparative expressed sequence hybridization to chromosomes for tumor classification and identification of genomic regions of differential gene expression
Evidence including region specific microarray analysis indicated that overexpression of several genes from a region may be required for detection by CESH, which is consistent with clusters of functionally related genes and mechanisms that affect the expression of a number of genes at a particular genomic location.
ICI D1694, an inhibitor of thymidylate synthase for clinical study.
The TS inhibitor, ICI D1694, is a highly potent inhibitor of tumour growth in vitro and in vivo. Uptake via the RFC and rapid metabolism to polyglutamate forms appear to be responsible for potency.