Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolatereductases from rat liver.
Brominated trimetrexate analogues as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolatereductase.
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolatereductase.
Ribbon diagram of human dihydrofolatereductase in complex with folate (blue).
Dihydrofolatereductase, or DHFR, reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry.
A variety of drugs act on dihydrofolatereductase, including the antibiotic trimethoprim, the antimalarial drug pyrimethamine, and the chemotherapeutic agents methotrexate and pemetrexed.
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