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.

Products
Background
Gene Data

Dihydrofolate Reductase Inhibitors

Cat. No. Product Name / Activity
1230 Methotrexate
Dihydrofolate reductase inhibitor
6185 Pemetrexed
High affinity dihydrofolate reductase inhibitor; also inhibits thymidylate synthase, GARFT and AICART
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.

External sources of pharmacological information for Dihydrofolate Reductase :

    Dihydrofolate Reductase Gene Data

    Species Gene Symbol Gene Accession No. Protein Accession No.
    Human DHFR NM_000791 P00374
    Mouse Dhfr NM_010049 P00375
    Rat Dhfr NM_130400 Q920D2