Dihydrofolate Reductase
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. DHFR has a key role in cell growth and proliferation.
Dihydrofolate Reductase Inhibitors |
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|---|---|
| Cat. No. | 产品名称/活性 |
| 1230 | Methotrexate |
| Dihydrofolate reductase inhibitor | |
| 6185 | Pemetrexed |
| High affinity dihydrofolate reductase inhibitor; also inhibits thymidylate synthase, GARFT and AICART | |
| 7362 | Phototrexate |
| Photoswitchable inhibitor of human dihydrofolate reductase | |
| 3918 | Pyrimethamine |
| DHFR inhibitor; also potent inhibitor of multidrug and toxin extrusion (MATE) transporters and STAT3 inhibitor | |
| 1592 | SCH 79797 dihydrochloride |
| Inhibits DHFR; also potent and selective PAR1 antagonist; broad spectrum antibiotic | |
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 regulated DHFR gene expression is controlled by Sp1 and E2F family transcription factors respectively and levels of this enzyme peak at the G1/S cell cycle boundary. Autoregulation, through DHFR-RNA interactions, has also been reported. The human gene encoding this enzyme is localized to 5q11.2-13.2.