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Glycinamide ribonucleotide transformylase (GARFTase) is a key folate-dependent enzyme in the de novo purine biosynthesis pathway. It catalyzes the transfer of a formyl group from 10-formyltetrahydrofolate to glycinamide ribonucleotide (GAR), producing formylglycinamide ribonucleotide (FGAR). This reaction is essential for the synthesis of purine nucleotides. As an essential enzyme for cell proliferation, GARFTase is an important target for antitumor drug design. Inhibition disrupts de novo purine synthesis leading to cytotoxicity especially in rapidly dividing cells such as cancer cells.
Inhibition of de novo purine synthesis
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