|Related Categories||1.5.x.x Acting on CH-NH, 1.x.x.x Oxidoreductases, Biochemicals and Reagents, Cell Biology, Enzyme Class Index,|
|form||ammonium sulfate suspension|
|activity||≥6 U/mg protein|
|density||1.2 g/mL at 20 °C|
In folate metabolism for the synthesis of purines, thymidine and glycine3
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1 U corresponds to the amount of enzyme which converts 1 μmol 7,8-dihydrofolate and NADPH to 5,6,7,8-tetrahydrofolate and NADP per minute at pH 6.5 and 25 °C
Suspension in 3.6 M ammonium sulfate solution, pH 7.0
Dihydrofolate reductase (DHFR) is involved in the synthesis of purines, thymidine and glycine in folate metabolism. DHFR, from bovine liver, is used for methotrexate analysis 1. DHFR is useful to study various cancers such as sarcomas, leukemias and head and neck cancers 2.
Dihydrofolate reductase (DHFR) reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as an electron donor. The binding of antitumor agents, such as methotrexate, to DHFR prevents the formation of reduced folates, which are essential for DNA synthesis 2.
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Keywords: Cell culture, Cell disruption, Cell signaling, Diagnostic, Digestions, Drug discovery, Functional genomics, Gene expression, Genomics, Metabolic Pathways, Molecular biology, Neuroscience, Proteomics
Evaluation of UDP-glucuronosyltransferase 2B17 (UGT2B17) and dihydrofolate reductase (DHFR) genes deletion and the expression level of NGX6 mRNA in breast cancer. Eskandari-Nasab E, Hashemi M, Rezaei H, et al. Mol. Biol. Rep. 39(12), 10531-9, (2012)
Association between expression of thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase and efficacy of pemetrexed in advanced non-small cell lung cancer. Shimizu T, Nakanishi Y, Nakagawa Y, et al. Anticancer Res. 32(10), 4589-96, (2012)
Mechanism of reversal of high glucose-induced endothelial nitric oxide synthase uncoupling by tanshinone IIA in human endothelial cell line EA.hy926. Zhou ZW, Xie XL, Zhou SF, et al. Eur. J. Pharmacol. 697(1-3), 97-105, (2012)
Mechanism-based design, synthesis and biological studies of N⁵-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents. Zhang Z, Tian C, Zhou S, et al. Eur. J. Med. Chem. 58, 228-36, (2012)
Sulfadoxine-pyrimethamine resistance in Plasmodium falciparum: a zoomed image at the molecular level within a geographic context. Abdul-Ghani R, Farag HF, and Allam AF Acta Trop. 125(2), 163-90, (2013)
Insulator-like pairing elements regulate silencing and mutually exclusive expression in the malaria parasite Plasmodium falciparum. Avraham I, Schreier J, and Dzikowski R Proc. Natl. Acad. Sci. U. S. A. 109(52), E3678-86, (2012)
Increased prevalence of dhfr and dhps mutants at delivery in Malawian pregnant women receiving intermittent preventive treatment for malaria. Lin JT, Mbewe B, Taylor SM, et al. Trop. Med. Int. Health 18(2), 175-8, (2013)
In vitro anti-Helicobacter pylori activity of a flavonoid rich extract of Glycyrrhiza glabra and its probable mechanisms of action. Asha MK, Debraj D, Prashanth D, et al. J. Ethnopharmacol. 145(2), 581-6, (2013)
A community-randomized evaluation of the effect of intermittent preventive treatment in infants on antimalarial drug resistance in southern Tanzania. Pearce RJ, Ord R, Kaur H, et al. J. Infect. Dis. 207(5), 848-59, (2013)
Interaction between Gambogic acid and dihydrofolate reductase and synergistic lethal effects with methotrexate on hepatoma cells. Deschatrette J, Ng-Bonaventure K, Philippe L, et al. Anticancer Res. 33(1), 133-42, (2013)
Crystal structures of Escherichia coli and Lactobacillus casei dihydrofolate reductase refined at 1.7 A resolution. I. General features and binding of methotrexate. Bolin JT, Filman DJ, Matthews DA, et al. J. Biol. Chem. 257(22), 13650-62, (1982)
Methotrexate-resistant variants of human dihydrofolate reductase with substitutions of leucine 22. Kinetics, crystallography, and potential as selectable markers. Lewis WS, Cody V, Galitsky N, et al. J. Biol. Chem. 270(10), 5057-64, (1995)
Dihydrofolate reductase deficiency due to a homozygous DHFR mutation causes megaloblastic anemia and cerebral folate deficiency leading to severe neurologic disease. Cario H, Smith DE, Blom H, et al. Am. J. Hum. Genet. 88(2), 226-31, (2011)
The former annotated human pseudogene dihydrofolate reductase-like 1 (DHFRL1) is expressed and functional. McEntee G, Minguzzi S, O'Brien K, et al. Proc. Natl. Acad. Sci. U. S. A. 108(37), 15157-62, (2011)
Human dihydrofolate reductase gene organization. Extensive conservation of the G + C-rich 5' non-coding sequence and strong intron size divergence from homologous mammalian genes. Yang JK, Masters JN, and Attardi G J. Mol. Biol. 176(2), 169-87, (1984)
Comparison of two independent crystal structures of human dihydrofolate reductase ternary complexes reduced with nicotinamide adenine dinucleotide phosphate and the very tight-binding inhibitor PT523. Cody V, Galitsky N, Luft JR, et al. Biochemistry 36(45), 13897-903, (1997)
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents. Gangjee A, Vidwans AP, Vasudevan A, et al. J. Med. Chem. 41(18), 3426-34, (1998)
Analysis of three crystal structure determinations of a 5-methyl-6-N-methylanilino pyridopyrimidine antifolate complex with human dihydrofolate reductase. Cody V, Luft JR, Pangborn W, et al. Acta Crystallogr. D, Biol. Crystallogr. 59(Pt 9), 1603-9, (2003)
Characterization and comparative studies of zebrafish and human recombinant dihydrofolate reductases--inhibition by folic acid and polyphenols. Kao TT, Wang KC, Chang WN, et al. Drug Metab. Dispos. 36(3), 508-16, (2008)
Multiple conformers in active site of human dihydrofolate reductase F31R/Q35E double mutant suggest structural basis for methotrexate resistance. Volpato JP, Yachnin BJ, Blanchet J, et al. J. Biol. Chem. 284(30), 20079-89, (2009)
Analysis of two polymorphic forms of a pyrido[2,3-d]pyrimidine N9-C10 reversed-bridge antifolate binary complex with human dihydrofolate reductase. Cody V, Galitsky N, Luft JR, et al. Acta Crystallogr. D, Biol. Crystallogr. 59(Pt 4), 654-61, (2003)
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents. Aleem Gangjee et al J. Med. Chem. 52, 4892-902, (2009)
Structure determination of tetrahydroquinazoline antifolates in complex with human and Pneumocystis carinii dihydrofolate reductase: correlations between enzyme selectivity and stereochemistry. Cody V, Luft JR, Pangborn W, et al. Acta Crystallogr. D, Biol. Crystallogr. 60(Pt 4), 646-55, (2004)
Understanding the role of Leu22 variants in methotrexate resistance: comparison of wild-type and Leu22Arg variant mouse and human dihydrofolate reductase ternary crystal complexes with methotrexate and NADPH. Cody V, Luft JR, and Pangborn W Acta Crystallogr. D, Biol. Crystallogr. 61(Pt 2), 147-55, (2005)
Correlations of inhibitor kinetics for Pneumocystis jirovecii and human dihydrofolate reductase with structural data for human active site mutant enzyme complexes. Cody V, Pace J, Makin J, et al. Biochemistry 48(8), 1702-11, (2009)
Atomic structures of human dihydrofolate reductase complexed with NADPH and two lipophilic antifolates at 1.09 a and 1.05 a resolution. Klon AE, Héroux A, Ross LJ, et al. J. Mol. Biol. 320(3), 677-93, (2002)
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