Dihydrofolate Reductase Inhibitors

Dihydrofolate reductase (DHFR) is a member of the reductase family of enzymes that is ubiquitously expressed in all organisms. It catalyzes tetrahydrofolate regeneration by reduction of dihydrofolate, using NADPH as a cofactor. Tetrahydrofolate is essential for de novo purine and thymidylate synthesis, hence DHFR has a critical role in cell growth and proliferation.

DHFR is the target for many cancer therapies including methotrexate because it is a key enzyme in cell replication. Basal and ...