In the past 65 years, antifolates targeting folate metabolism played a pivotal role in drug
treatment of malignant, microbial, parasitic and chronic inflammatory diseases. Drug
discovery of novel antifolates with improved properties and superior activities remains an
attractive strategy both in academia and in the pharmaceutical industry. Among novel
antifolates are pemetrexed which primarily targets thymidylate synthase as well as
pralatrexate which blocks dihydrofolate reductase, and displays enhanced transport and …