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Formyltransferases are key enzymes in the *de novo* purine biosynthetic pathway, responsible for transferring formyl groups during the multi-step synthesis of purine nucleotides. These enzymes utilize tetrahydrofolate derivatives as one-carbon donors and are essential for building the purine ring structure that ultimately forms inosine monophosphate (IMP), a precursor to both adenine and guanine nucleotides. In humans, both GAR and AICAR transformylase activities reside within a bifunctional enzyme called ATIC. Inhibition of these enzymes disrupts nucleotide balance and impairs DNA/RNA synthesis, making them therapeutic targets, particularly in cancer.
Inhibition of formyl transfer, leading to disruption of purine nucleotide synthesis
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