Folate analogues function by inhibiting enzymes necessary for DNA and RNA synthesis. One of the most well-known folate analogues, methotrexate, inhibits the enzyme dihydrofolate reductase (DHFR), which is essential for the conversion of dihydrofolate to tetrahydrofolate, a precursor in the synthesis of thymidylate and purines. By blocking this pathway, methotrexate prevents the formation of DNA, thereby inhibiting cell division and growth of cancer cells.
