Leucovorin provides a source of the tetrahydrofolates that are depleted by methotrexate's inhibition of dihydrofolate reductase
, but methotrexate competes with leucovorin for cell uptake.
Molecular epidemiology of Plasmodium falciparum antifolate resistance in Vietnam: genotyping for resistance variants of dihydropteroate synthase and dihydrofolate reductase
Polymorphisms in the dihydrofolate reductase
(DHFR) and dihydropteroate synthetase (DHPS) genes of Plasmodium falciparum and in vivo resistance to sulphadoxine/pyrimethamine in isolates from Tanzania.
The drug works by inhibiting the activity of an enzyme, dihydrofolate reductase
(DHFR), that is instrumental in the synthesis of a DNA precursor necessary for cell reproduction.
Key classes of mechanism of action includes Interleukin inhibitors, Kinase inhibitors, cytokine targetters, TNF targetters, C5a receptor antagonists, Cathepsin inhibitors, Histone deacetylase inhibitors (HDAC) inhibitors, Janus Kinase 3(JAK-3) inhibitors, CD4 inhibitors, p38 kinase inhibitors, Dihydrofolate Reductase
inhibitors, cyclooxygenase (COX) inhibitors, Chemokine receptor antagonists, Glucocorticoid antagonists, Dihydroorotate dehydrogenase(DHODH) inhibitors, and combination therapies.
Investigators have taken advantage of the property of MTX to inhibit the enzyme dihydrofolate reductase
(DHFR), an important enzyme that catalyzes the reduction of dihydrofolate to tetrahydrofolate in the presence of NADPH (18-20).
For example, at the AAAS meeting scientists described work with an enzyme, dihydrofolate reductase
(DHFR), that is essential to nucleic acid synthesis and cell growth.
Pralatrexate is a novel, small molecule chemotherapeutic agent that inhibits dihydrofolate reductase
, or DHFR, a folic acid (folate)-dependent enzyme involved in the building of nucleic acid, or DNA, and other processes.
The DHFR-/- CHO line was developed through CompoZr ZFN mediated gene editing of the dihydrofolate reductase
(DHFR) locus in a robust, extensively characterized and fully documented CHO-K1 host.
Sequencing of the dihydrofolate reductase
(pfdhfr) and dihydropoteroate synthase (pfdhps) genes (online Technical Appendix Table) detected 4 SNPs in pfdhfr associated with pyrimethamine resistance (N51I, C59R, S108N, and I164L) and 4 SNPs in pfdhps associated with sulfadoxine resistance (S436A, A437G, K540E/N, and A581G) (Table 1).
The folic acid analog methotrexate (MTX)  inhibits the enzyme dihydrofolate reductase
(DHFR; EC 1.
Iclaprim was designed to meet a growing medical need for additional treatment options to combat resistant infections and is the first antibiotic in the dihydrofolate reductase
(DHFR) selective inhibitor class to demonstrate efficacy against cSSSIs caused by MRSA.