Nolatrexed dihydrochloride is a water-soluble lipophilic quinazoline folate analog that exhibits potent antineoplastic activity. Nolatrexed is a potent thymidylate synthase inhibitor that inhibits thymine synthesis followed by inhibition of DNA replication.
British journal of cancer, 82(9), 1519-1527 (2000-05-02)
A clinical study of nolatrexed dihydrochloride (AG337, Thymitaq) in combination with paclitaxel was performed. The aims were to optimize the schedule of administration and determine any pharmacokinetic (PK) interactions between the two drugs. In vitro combination studies were performed to
The Journal of biological chemistry, 291(47), 24768-24778 (2016-10-21)
The aim of this study was to identify and characterize mechanisms of resistance to antifolate drugs in African trypanosomes. Genome-wide RNAi library screens were undertaken in bloodstream form Trypanosoma brucei exposed to the antifolates methotrexate and raltitrexed. In conjunction with
The Journal of biological chemistry, 292(32), 13449-13458 (2017-06-22)
Thymidylate synthase (TS) is the sole enzyme responsible for de novo biosynthesis of thymidylate (TMP) and is essential for cell proliferation and survival. Inhibition of human TS (hTS) has been extensively investigated for cancer chemotherapy, but several aspects of its
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