This webpage contains legacy information. The product is either no longer available from the supplier or has been delisted at Labome.
product summary
company name :
MilliporeSigma
other brands :
FLUKA, Sigma-Aldrich, Roche Applied Science
product type :
protein
product name :
Dihydrofolate Reductase human
catalog :
D6566
citations: 92
Reference
Hopper A, Brockman A, Wise A, Gould J, Barks J, Radke J, et al. Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis. J Med Chem. 2019;62:1562-1576 pubmed publisher
Xu F, Sudo Y, Sanechika S, Yamashita J, Shimaguchi S, Honda S, et al. Disturbed biopterin and folate metabolism in the Qdpr-deficient mouse. FEBS Lett. 2014;588:3924-31 pubmed publisher
Oyen D, Steyaert J, Barlow J. Inhibition of ligand exchange kinetics via active-site trapping with an antibody fragment. Biochemistry. 2014;53:1879-81 pubmed publisher
Iqbal M, Burney I. Low doses of colony-stimulating factors lead to resolution of neutropenia in cancer patients through increased levels of dihydrofolate reductase. Pak J Pharm Sci. 2014;27:245-8 pubmed
G Dayanandan N, Paulsen J, Viswanathan K, Keshipeddy S, Lombardo M, Zhou W, et al. Propargyl-linked antifolates are dual inhibitors of Candida albicans and Candida glabrata. J Med Chem. 2014;57:2643-56 pubmed publisher
Bhojane P, Duff M, Patel H, Vogt M, Howell E. Investigation of osmolyte effects on FolM: comparison with other dihydrofolate reductases. Biochemistry. 2014;53:1330-41 pubmed publisher
Fenwick R, van den Bedem H, Fraser J, Wright P. Integrated description of protein dynamics from room-temperature X-ray crystallography and NMR. Proc Natl Acad Sci U S A. 2014;111:E445-54 pubmed publisher
Pereira L, Baroni L, Yatsuda A. A transgenic Neospora caninum strain based on mutations of the dihydrofolate reductase-thymidylate synthase gene. Exp Parasitol. 2014;138:40-7 pubmed publisher
Lam T, Hilgers M, Cunningham M, Kwan B, Nelson K, Brown Driver V, et al. Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines. J Med Chem. 2014;57:651-68 pubmed publisher
Sharon E, Volchek L, Frenkel N. Human herpesvirus 6 (HHV-6) alters E2F1/Rb pathways and utilizes the E2F1 transcription factor to express viral genes. Proc Natl Acad Sci U S A. 2014;111:451-6 pubmed publisher
Francis K, Stojković V, Kohen A. Preservation of protein dynamics in dihydrofolate reductase evolution. J Biol Chem. 2013;288:35961-8 pubmed publisher
Chen S, Fahmi N, Bhattacharya C, Wang L, Jin Y, Benkovic S, et al. Fluorescent biphenyl derivatives of phenylalanine suitable for protein modification. Biochemistry. 2013;52:8580-9 pubmed publisher
Ohmae E, Miyashita Y, Tate S, Gekko K, Kitazawa S, Kitahara R, et al. Solvent environments significantly affect the enzymatic function of Escherichia coli dihydrofolate reductase: comparison of wild-type protein and active-site mutant D27E. Biochim Biophys Acta. 2013;1834:2782-94 pubmed publisher
Bhabha G, Ekiert D, Jennewein M, Zmasek C, Tuttle L, Kroon G, et al. Divergent evolution of protein conformational dynamics in dihydrofolate reductase. Nat Struct Mol Biol. 2013;20:1243-9 pubmed publisher
Jiang P, Corbett Detig R, Hartl D, Lozovsky E. Accessible mutational trajectories for the evolution of pyrimethamine resistance in the malaria parasite Plasmodium vivax. J Mol Evol. 2013;77:81-91 pubmed publisher
Luk L, Javier Ruiz Pernía J, Dawson W, Roca M, Loveridge E, Glowacki D, et al. Unraveling the role of protein dynamics in dihydrofolate reductase catalysis. Proc Natl Acad Sci U S A. 2013;110:16344-9 pubmed publisher
Hartl F, Hayer Hartl M. The first chaperonin. Nat Rev Mol Cell Biol. 2013;14:611 pubmed publisher
Sharma H, Landau M, Vargo M, Spasov K, Anderson K. First three-dimensional structure of Toxoplasma gondii thymidylate synthase-dihydrofolate reductase: insights for catalysis, interdomain interactions, and substrate channeling. Biochemistry. 2013;52:7305-7317 pubmed publisher
Lamb K, G Dayanandan N, Wright D, Anderson A. Elucidating features that drive the design of selective antifolates using crystal structures of human dihydrofolate reductase. Biochemistry. 2013;52:7318-26 pubmed publisher
Arinaitwe E, Ades V, Walakira A, Ninsiima B, Mugagga O, Patil T, et al. Intermittent preventive therapy with sulfadoxine-pyrimethamine for malaria in pregnancy: a cross-sectional study from Tororo, Uganda. PLoS ONE. 2013;8:e73073 pubmed publisher
Wilson M. Visualizing networks of mobility in proteins. Nat Methods. 2013;10:835-7 pubmed publisher
Chen S, Fahmi N, Wang L, Bhattacharya C, Benkovic S, Hecht S. Detection of dihydrofolate reductase conformational change by FRET using two fluorescent amino acids. J Am Chem Soc. 2013;135:12924-7 pubmed publisher
Miyajima M, Minoshima M, Tanaka M, Nishimura R, Hishioka N, Numata T, et al. Increase in tetrahydrobiopterin concentration with aging in the cerebral cortex of the senescence-accelerated mouse prone 10 strain caused by abnormal regulation of tetrahydrobiopterin biosynthesis. Biogerontology. 2013;14:491-501 pubmed publisher
Mita T, Ohashi J, Venkatesan M, Marma A, Nakamura M, Plowe C, et al. Ordered accumulation of mutations conferring resistance to sulfadoxine-pyrimethamine in the Plasmodium falciparum parasite. J Infect Dis. 2014;209:130-9 pubmed publisher
van den Bedem H, Bhabha G, Yang K, Wright P, Fraser J. Automated identification of functional dynamic contact networks from X-ray crystallography. Nat Methods. 2013;10:896-902 pubmed publisher
Oyen D, Wechselberger R, Srinivasan V, Steyaert J, Barlow J. Mechanistic analysis of allosteric and non-allosteric effects arising from nanobody binding to two epitopes of the dihydrofolate reductase of Escherichia coli. Biochim Biophys Acta. 2013;1834:2147-57 pubmed publisher
Marverti G, Ligabue A, Lombardi P, Ferrari S, Monti M, Frassineti C, et al. Modulation of the expression of folate cycle enzymes and polyamine metabolism by berberine in cisplatin-sensitive and -resistant human ovarian cancer cells. Int J Oncol. 2013;43:1269-80 pubmed publisher
Too P, Erales J, Simen J, Marjanovic A, Coffino P. Slippery substrates impair function of a bacterial protease ATPase by unbalancing translocation versus exit. J Biol Chem. 2013;288:13243-57 pubmed publisher
Weichenberger C, Pozharski E, Rupp B. Visualizing ligand molecules in Twilight electron density. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2013;69:195-200 pubmed publisher
Miller J, Chu Y, Castaneda L, Serrano K, Brooks R, Heistad D. Vascular function during prolonged progression and regression of atherosclerosis in mice. Arterioscler Thromb Vasc Biol. 2013;33:459-65 pubmed publisher
Ding S, Ye R, Zhang D, Sun X, Zhou H, McCutchan T, et al. Anti-folate combination therapies and their effect on the development of drug resistance in Plasmodium vivax. Sci Rep. 2013;3:1008 pubmed publisher
Ng S, Tan T, Wang Y, Ng D, Goh L, Bardor M, et al. Production of functional soluble Dectin-1 glycoprotein using an IRES-linked destabilized-dihydrofolate reductase expression vector. PLoS ONE. 2012;7:e52785 pubmed publisher
Deschatrette J, Ng Bonaventure K, Philippe L, Wolfrom C. Interaction between Gambogic acid and dihydrofolate reductase and synergistic lethal effects with methotrexate on hepatoma cells. Anticancer Res. 2013;33:133-42 pubmed
Pearce R, Ord R, Kaur H, Lupala C, Schellenberg J, Shirima K, et al. A community-randomized evaluation of the effect of intermittent preventive treatment in infants on antimalarial drug resistance in southern Tanzania. J Infect Dis. 2013;207:848-59 pubmed publisher
Asha M, Debraj D, Prashanth D, Edwin J, Srikanth H, Muruganantham N, et al. In vitro anti-Helicobacter pylori activity of a flavonoid rich extract of Glycyrrhiza glabra and its probable mechanisms of action. J Ethnopharmacol. 2013;145:581-6 pubmed publisher
Bershtein S, Mu W, Serohijos A, Zhou J, Shakhnovich E. Protein quality control acts on folding intermediates to shape the effects of mutations on organismal fitness. Mol Cell. 2013;49:133-44 pubmed publisher
Lin J, Mbewe B, Taylor S, Luntamo M, Meshnick S, Ashorn P. Increased prevalence of dhfr and dhps mutants at delivery in Malawian pregnant women receiving intermittent preventive treatment for malaria. Trop Med Int Health. 2013;18:175-8 pubmed publisher
Avraham I, Schreier J, Dzikowski R. Insulator-like pairing elements regulate silencing and mutually exclusive expression in the malaria parasite Plasmodium falciparum. Proc Natl Acad Sci U S A. 2012;109:E3678-86 pubmed publisher
Hsieh Y, Tedeschi P, Adebisi Lawal R, Banerjee D, SCOTTO K, Kerrigan J, et al. Enhanced degradation of dihydrofolate reductase through inhibition of NAD kinase by nicotinamide analogs. Mol Pharmacol. 2013;83:339-53 pubmed publisher
Hoang H, Padgham S, Meininger C. L-arginine, tetrahydrobiopterin, nitric oxide and diabetes. Curr Opin Clin Nutr Metab Care. 2013;16:76-82 pubmed publisher
Chumakov S, Kravchenko I, Chumakov P. [Protein complementation as tool for studying protein-protein interactions in living cells]. Mol Biol (Mosk). 2012;46:699-711 pubmed
Belmonte L, Pechkova E, Tripathi S, Scudieri D, Nicolini C. Langmuir-Blodgett nanotemplate and radiation resistance in protein crystals: state of the art. Crit Rev Eukaryot Gene Expr. 2012;22:219-32 pubmed
Abdul Ghani R, Farag H, Allam A. Sulfadoxine-pyrimethamine resistance in Plasmodium falciparum: a zoomed image at the molecular level within a geographic context. Acta Trop. 2013;125:163-90 pubmed publisher
Zhang Z, Tian C, Zhou S, Wang W, Guo Y, Xia J, et al. Mechanism-based design, synthesis and biological studies of N⁵-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents. Eur J Med Chem. 2012;58:228-36 pubmed publisher
Chen S, Wang L, Fahmi N, Benkovic S, Hecht S. Two pyrenylalanines in dihydrofolate reductase form an excimer enabling the study of protein dynamics. J Am Chem Soc. 2012;134:18883-5 pubmed publisher
Genheden S. Are homology models sufficiently good for free-energy simulations?. J Chem Inf Model. 2012;52:3013-21 pubmed publisher
Freschi L, Torres Quiroz F, Dubé A, Landry C. qPCA: a scalable assay to measure the perturbation of protein-protein interactions in living cells. Mol Biosyst. 2013;9:36-43 pubmed publisher
Martinelli M, Scapoli L, Carbonara P, Valentini I, Girardi A, Farinella F, et al. Idiopathic pulmonary fibrosis and polymorphisms of the folate pathway genes. Clin Biochem. 2013;46:85-8 pubmed publisher
Wang W, Gao J, Wang J, Liu C, Meng Y. Cloning, expression and enzymatic properties analysis of dihydrofolate reductase gene from the silkworm, Bombyx mori. Mol Biol Rep. 2012;39:10285-91 pubmed publisher
Zhou Z, Xie X, Zhou S, Li C. Mechanism of reversal of high glucose-induced endothelial nitric oxide synthase uncoupling by tanshinone IIA in human endothelial cell line EA.hy926. Eur J Pharmacol. 2012;697:97-105 pubmed publisher
Shimizu T, Nakanishi Y, Nakagawa Y, Tsujino I, Takahashi N, Nemoto N, et al. Association between expression of thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase and efficacy of pemetrexed in advanced non-small cell lung cancer. Anticancer Res. 2012;32:4589-96 pubmed
Eskandari Nasab E, Hashemi M, Rezaei H, Fazaeli A, Mashhadi M, Moghaddam S, et al. Evaluation of UDP-glucuronosyltransferase 2B17 (UGT2B17) and dihydrofolate reductase (DHFR) genes deletion and the expression level of NGX6 mRNA in breast cancer. Mol Biol Rep. 2012;39:10531-9 pubmed publisher
Hayashi H, Tazoe Y, Horino M, Fujimaki Katoh C, Tsuboi S, Matsuyama T, et al. An artifact derived from a pseudogene led to the discovery of microRNA binding site polymorphism in the 3'-untranslated region of the human dihydrofolate reductase gene. Drug Metab Pharmacokinet. 2012;27:263-7 pubmed
Asada M, Tanaka M, Goto Y, Yokoyama N, Inoue N, Kawazu S. Stable expression of green fluorescent protein and targeted disruption of thioredoxin peroxidase-1 gene in Babesia bovis with the WR99210/dhfr selection system. Mol Biochem Parasitol. 2012;181:162-70 pubmed publisher
Evangelopoulos D, Cronin N, Daviter T, Sim E, Keep N, Bhakta S. Characterization of an oxidoreductase from the arylamine N-acetyltransferase operon in Mycobacterium smegmatis. FEBS J. 2011;278:4824-32 pubmed publisher
Cody V, Pace J, Nowak J. Structural analysis of human dihydrofolate reductase as a binary complex with the potent and selective inhibitor 2,4-diamino-6-{2'-O-(3-carboxypropyl)oxydibenz[b,f]-azepin-5-yl}methylpteridine reveals an unusual binding mode. Acta Crystallogr D Biol Crystallogr. 2011;67:875-80 pubmed publisher
Anderson D, Quintero C, Stover P. Identification of a de novo thymidylate biosynthesis pathway in mammalian mitochondria. Proc Natl Acad Sci U S A. 2011;108:15163-8 pubmed publisher
McEntee G, Minguzzi S, O Brien K, Ben Larbi N, Loscher C, Ó Fágáin C, et al. The former annotated human pseudogene dihydrofolate reductase-like 1 (DHFRL1) is expressed and functional. Proc Natl Acad Sci U S A. 2011;108:15157-62 pubmed publisher
Cario H, Smith D, Blom H, Blau N, Bode H, Holzmann K, et al. Dihydrofolate reductase deficiency due to a homozygous DHFR mutation causes megaloblastic anemia and cerebral folate deficiency leading to severe neurologic disease. Am J Hum Genet. 2011;88:226-31 pubmed publisher
Banka S, Blom H, Walter J, Aziz M, Urquhart J, Clouthier C, et al. Identification and characterization of an inborn error of metabolism caused by dihydrofolate reductase deficiency. Am J Hum Genet. 2011;88:216-25 pubmed publisher
Burkard T, Planyavsky M, Kaupe I, Breitwieser F, Burckstummer T, Bennett K, et al. Initial characterization of the human central proteome. BMC Syst Biol. 2011;5:17 pubmed publisher
Kaur J, Kumar P, Tyagi S, Pathak R, Batra S, Singh P, et al. In silico screening, structure-activity relationship, and biologic evaluation of selective pteridine reductase inhibitors targeting visceral leishmaniasis. Antimicrob Agents Chemother. 2011;55:659-66 pubmed publisher
Sánchez del Campo L, Sáez Ayala M, Chazarra S, Cabezas Herrera J, Rodriguez Lopez J. Binding of natural and synthetic polyphenols to human dihydrofolate reductase. Int J Mol Sci. 2009;10:5398-410 pubmed publisher
Gangjee A, Li W, Kisliuk R, Cody V, Pace J, Piraino J, et al. 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. J Med Chem. 2009;52:4892-902 pubmed publisher
Volpato J, Yachnin B, Blanchet J, Guerrero V, Poulin L, Fossati E, et al. Multiple conformers in active site of human dihydrofolate reductase F31R/Q35E double mutant suggest structural basis for methotrexate resistance. J Biol Chem. 2009;284:20079-89 pubmed publisher
Cody V, Pace J, Makin J, Piraino J, Queener S, Rosowsky A. Correlations of inhibitor kinetics for Pneumocystis jirovecii and human dihydrofolate reductase with structural data for human active site mutant enzyme complexes. Biochemistry. 2009;48:1702-11 pubmed publisher
Kao T, Wang K, Chang W, Lin C, Chen B, Wu H, et al. Characterization and comparative studies of zebrafish and human recombinant dihydrofolate reductases--inhibition by folic acid and polyphenols. Drug Metab Dispos. 2008;36:508-16 pubmed
Bechtel S, Rosenfelder H, Duda A, Schmidt C, Ernst U, Wellenreuther R, et al. The full-ORF clone resource of the German cDNA Consortium. BMC Genomics. 2007;8:399 pubmed publisher
Reynolds R, Campbell S, Fairchild R, Kisliuk R, Micca P, Queener S, et al. Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation. J Med Chem. 2007;50:3283-9 pubmed
Kovalevskaya N, Smurnyy Y, Polshakov V, Birdsall B, Bradbury A, Frenkiel T, et al. Solution structure of human dihydrofolate reductase in its complex with trimethoprim and NADPH. J Biomol NMR. 2005;33:69-72 pubmed
Cody V, Luft J, Pangborn W. 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. Acta Crystallogr D Biol Crystallogr. 2005;61:147-55 pubmed
Gerhard D, Wagner L, Feingold E, Shenmen C, Grouse L, Schuler G, et al. The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004;14:2121-7 pubmed
Schmutz J, Martin J, Terry A, Couronne O, Grimwood J, Lowry S, et al. The DNA sequence and comparative analysis of human chromosome 5. Nature. 2004;431:268-74 pubmed
Cody V, Luft J, Pangborn W, Gangjee A, Queener S. Structure determination of tetrahydroquinazoline antifolates in complex with human and Pneumocystis carinii dihydrofolate reductase: correlations between enzyme selectivity and stereochemistry. Acta Crystallogr D Biol Crystallogr. 2004;60:646-55 pubmed
Cody V, Luft J, Pangborn W, Gangjee A. Analysis of three crystal structure determinations of a 5-methyl-6-N-methylanilino pyridopyrimidine antifolate complex with human dihydrofolate reductase. Acta Crystallogr D Biol Crystallogr. 2003;59:1603-9 pubmed
Cody V, Galitsky N, Luft J, Pangborn W, Gangjee A. Analysis of two polymorphic forms of a pyrido[2,3-d]pyrimidine N9-C10 reversed-bridge antifolate binary complex with human dihydrofolate reductase. Acta Crystallogr D Biol Crystallogr. 2003;59:654-61 pubmed
Klon A, Heroux A, Ross L, Pathak V, Johnson C, Piper J, et al. Atomic structures of human dihydrofolate reductase complexed with NADPH and two lipophilic antifolates at 1.09 a and 1.05 a resolution. J Mol Biol. 2002;320:677-93 pubmed
Gangjee A, Vidwans A, Vasudevan A, Queener S, Kisliuk R, Cody V, et al. 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. J Med Chem. 1998;41:3426-34 pubmed
Cody V, Galitsky N, Luft J, Pangborn W, Rosowsky A, Blakley R. 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. Biochemistry. 1997;36:13897-903 pubmed
Blakley R. Eukaryotic dihydrofolate reductase. Adv Enzymol Relat Areas Mol Biol. 1995;70:23-102 pubmed
Lewis W, Cody V, Galitsky N, Luft J, Pangborn W, Chunduru S, et al. Methotrexate-resistant variants of human dihydrofolate reductase with substitutions of leucine 22. Kinetics, crystallography, and potential as selectable markers. J Biol Chem. 1995;270:5057-64 pubmed
Gready J. Dihydrofolate reductase: binding of substrates and inhibitors and catalytic mechanism. Adv Pharmacol Chemother. 1980;17:37-102 pubmed
Bolin J, Filman D, Matthews D, Hamlin R, Kraut J. Crystal structures of Escherichia coli and Lactobacillus casei dihydrofolate reductase refined at 1.7 A resolution. I. General features and binding of methotrexate. J Biol Chem. 1982;257:13650-62 pubmed
Masters J, Attardi G. The nucleotide sequence of the cDNA coding for the human dihydrofolic acid reductase. Gene. 1983;21:59-63 pubmed
Chen M, Shimada T, Moulton A, Cline A, Humphries R, Maizel J, et al. The functional human dihydrofolate reductase gene. J Biol Chem. 1984;259:3933-43 pubmed
Yang J, Masters J, Attardi G. 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. J Mol Biol. 1984;176:169-87 pubmed
Kaufman B, Gardiner R. Studies on dihydrofolic reductase. I. Purification and properties of dihydrofolic reductase from chicken liver. J Biol Chem. 1966;241:1319-28 pubmed
Young I, Gibson F. Regulation of the enzymes involved in the biosynthesis of 2,3-dihydroxybenzoic acid in Aerobacter aerogenes and Escherichia coli. Biochim Biophys Acta. 1969;177:401-11 pubmed
Oefner C, D Arcy A, Winkler F. Crystal structure of human dihydrofolate reductase complexed with folate. Eur J Biochem. 1988;174:377-85 pubmed
Davies J, Delcamp T, Prendergast N, Ashford V, Freisheim J, Kraut J. Crystal structures of recombinant human dihydrofolate reductase complexed with folate and 5-deazafolate. Biochemistry. 1990;29:9467-79 pubmed
Schweitzer B, Dicker A, Bertino J. Dihydrofolate reductase as a therapeutic target. FASEB J. 1990;4:2441-52 pubmed
Stockman B, Nirmala N, Wagner G, Delcamp T, DeYarman M, Freisheim J. Sequence-specific 1H and 15N resonance assignments for human dihydrofolate reductase in solution. Biochemistry. 1992;31:218-29 pubmed
product information
Catalog Number :
D6566
Product Name :
Dihydrofolate Reductase human
Product Type :
PROTEINS & ENZYMES
Product Group :
Protein & Pathway Technologies
Product Description :
≥80% (SDS-PAGE), recombinant, expressed in E. coli,
company information
MilliporeSigma
PO Box 14508
St. Louis, MO 63178
https://www.sigmaaldrich.com
1-800-325-3010
headquarters: USA