Page last updated: 2024-09-03

wr 99210 and pyrimethamine

wr 99210 has been researched along with pyrimethamine in 28 studies

Compound Research Comparison

Studies
(wr 99210)
Trials
(wr 99210)
Recent Studies (post-2010)
(wr 99210)
Studies
(pyrimethamine)
Trials
(pyrimethamine)
Recent Studies (post-2010) (pyrimethamine)
590125,0887381,047

Protein Interaction Comparison

ProteinTaxonomywr 99210 (IC50)pyrimethamine (IC50)
Dihydrofolate reductaseHomo sapiens (human)3.1057
Dihydrofolate reductase Bos taurus (cattle)0.1007
Beta-hexosaminidase subunit alphaHomo sapiens (human)6.8333
Beta-hexosaminidase subunit betaHomo sapiens (human)6.4
Dihydrofolate reductaseEscherichia coli K-124.3
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K10.0609
Dihydrofolate reductasePneumocystis carinii3.25
Dihydrofolate reductaseCandida albicans5
Low molecular weight phosphotyrosine protein phosphataseHomo sapiens (human)15.615
Dipeptidyl peptidase 4Homo sapiens (human)0.39
Bifunctional dihydrofolate reductase-thymidylate synthaseToxoplasma gondii0.3217
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum 3D72.48
Dihydrofolate reductaseRattus norvegicus (Norway rat)2.0727

Research

Studies (28)

TimeframeStudies, this research(%)All Research%
pre-19904 (14.29)18.7374
1990's3 (10.71)18.2507
2000's18 (64.29)29.6817
2010's3 (10.71)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Genther, CS; Smith, CS1
Ager, AL; Bliss, RA; Canfield, CJ; Jacobus, DP; Jensen, NP; Kotecka, BM; Rieckmann, KH; Terpinski, J1
Chitnumsub, P; Kamchonwongpaisan, S; Sirawaraporn, W; Taylor, P; Vanichtanankul, J; Walkinshaw, MD; Yuthavong, Y; Yuvaniyama, J1
Ferrari, AM; Pacchioni, S; Parenti, MD; Rastelli, G1
Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; O'Neil, MT; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, PL; Yang, YS1
Chusacultanachai, S; Japrung, D; Leartsakulpanich, U; Yuthavong, Y1
Borrmann, S; Kiara, SM; Masseno, V; Mwai, L; Nzila, A; Ochola, I; Okombo, J1
Brun, R; Chitnumsub, P; Dartois, V; Diagana, TT; Goh, A; Kamchonwongpaisan, S; Keller, TH; Kiara, SM; Lakshminarayana, SB; Ma, NL; Maneeruttanarungroj, C; Nzila, A; Rottmann, M; Taweechai, S; Weaver, M; Wittlin, S; Wong, J; Yeung, BK; Yuthavong, Y; Zou, B1
Adams, JH; Auliff, AM; Cheng, Q; O'Neil, MT1
Childs, GE; Pooyindee, N; Wimonwattrawatee, T1
Howells, RE; Judge, BM1
Knight, DJ; Williamson, P1
Hartwell, LH; Sibley, CH; Vasquez, B; Wooden, JM1
Hekmat-Nejad, M; Rathod, PK1
Howard, V; Mookherjee, S; Nzila-Mouanda, A; Sibley, CH; Watkins, W1
de Koning-Ward, TF; Fidock, DA; Janse, CJ; Menard, R; Thathy, V; van Spaendonk, RM; Waters, AP1
Kamchonwongpaisan, S; Lowe, G; Quarrell, R; Rastelli, G; Sirawaraporn, W; Sompornpisut, P; Thebtaranonth, Y; Vilaivan, T; Yuthavong, Y1
Hankins, EG; Sibley, CH; Warhurst, DC1
Delfino, RT; Figueroa-Villar, JD; Santos-Filho, OA1
Jia, Q; Kovacs, JA; Ma, L1
Hastings, MD; Sibley, CH1
de Vries, E; Franssen, FF; Gaffar, FR; Wilschut, K1
Hyde, JE; Nirmalan, N; Sims, PF1
Hunt, SY; Rezvani, BB; Sibley, CH1
Anh, le N; Auliff, A; Bell, D; Chen, N; Cheng, Q; Gao, Q; Maguire, J; O'Neil, MT; Russell, B; Wilson, DW1
Chitnumsub, P; Kamchonwongpaisan, S; Taweechai, S; Vanichtanankul, J; Yuthavong, Y1
Janse, CJ; Ramesar, J; Waters, AP1
Adams, JH; Auliff, AM; Balu, B; Chen, N; Cheng, Q; O'Neil, MT1

Other Studies

28 other study(ies) available for wr 99210 and pyrimethamine

ArticleYear
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
    Journal of medicinal chemistry, 1977, Volume: 20, Issue:2

    Topics: Animals; Antimalarials; Bacteria; Drug Resistance, Microbial; Escherichia coli; Folic Acid; Folic Acid Antagonists; Malaria; Mice; Plasmodium berghei; Triazines

1977
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
    Journal of medicinal chemistry, 2001, Nov-08, Volume: 44, Issue:23

    Topics: Animals; Antimalarials; Drug Evaluation, Preclinical; Female; Folic Acid Antagonists; Guanidines; Malaria; Male; Mice; Plasmodium berghei; Plasmodium falciparum; Prodrugs; Proguanil; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2001
Insights into antifolate resistance from malarial DHFR-TS structures.
    Nature structural biology, 2003, Volume: 10, Issue:5

    Topics: Amino Acid Sequence; Animals; Conserved Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Multienzyme Complexes; Plasmodium; Plasmodium falciparum; Protein Conformation; Sequence Alignment; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase

2003
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
    Journal of medicinal chemistry, 2004, Aug-12, Volume: 47, Issue:17

    Topics: Aldehyde Reductase; Animals; Antimalarials; Binding Sites; Folic Acid Antagonists; Models, Molecular; Plasmodium falciparum; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase

2004
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
    Journal of medicinal chemistry, 2005, Apr-21, Volume: 48, Issue:8

    Topics: Animals; Antimalarials; Biguanides; Chromatography, Liquid; Drug Resistance; Folic Acid Antagonists; Humans; In Vitro Techniques; Mass Spectrometry; Microsomes, Liver; Plasmodium falciparum; Prodrugs; Structure-Activity Relationship; Triazines

2005
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
    Antimicrobial agents and chemotherapy, 2007, Volume: 51, Issue:12

    Topics: Animals; Antimalarials; Drug Resistance; Drug Resistance, Multiple; Kinetics; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2007
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:9

    Topics: Animals; Antimalarials; Folic Acid Antagonists; Genotype; Inhibitory Concentration 50; Kenya; Methotrexate; Mutation; Plasmodium falciparum; Polymerase Chain Reaction; Polymorphism, Genetic; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim; Trimetrexate

2009
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Administration, Oral; Animals; Antimalarials; Biological Availability; Drug Resistance; Female; Folic Acid Antagonists; Humans; In Vitro Techniques; Malaria; Malaria, Falciparum; Male; Mice; Models, Molecular; Mutation; Parasitic Sensitivity Tests; Plasmodium berghei; Plasmodium falciparum; Pyrimethamine; Quinazolines; Rats; Rats, Wistar; Tetrahydrofolate Dehydrogenase

2010
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:9

    Topics: Animals; Folic Acid Antagonists; Multienzyme Complexes; Mutation; Parasitic Sensitivity Tests; Plasmodium falciparum; Plasmodium vivax; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection

2010
Evaluation of an in vitro assay system for drug susceptibility of field isolates of Plasmodium falciparum from southern Thailand.
    The American journal of tropical medicine and hygiene, 1988, Volume: 38, Issue:1

    Topics: Amodiaquine; Animals; Antimalarials; Butylated Hydroxytoluene; Chloroquine; Humans; Mefloquine; Parasitology; Phenanthrenes; Plasmodium falciparum; Pyridines; Pyrimethamine; Quinine; Quinolines; Thailand; Triazines

1988
Sustained-release implants in the chemotherapy of experimental rodent malaria I. A comparison of the effects of some antimalarials in polydimethylsiloxane matrices.
    Annals of tropical medicine and parasitology, 1981, Volume: 75, Issue:5

    Topics: Animals; Antimalarials; Chloroquine; Dimethylpolysiloxanes; Drug Implants; Malaria; Male; Mefloquine; Mice; Mice, Inbred Strains; Naphthoquinones; Piperidines; Plasmodium berghei; Primaquine; Proguanil; Pyrimethamine; Quinolines; Silicone Elastomers; Sulfadiazine; Triazines

1981
The antimalarial activity of N-benzyl-oxydihydrotriazines. IV. The development of resistance to BRL 6231 (4,6-diamino-1,2-dihyydro-2-,2-dimethyl-1-(2,4,5-trichloropropyloxy)-1,3,5 triazine hydrochloride) by Plasmodium berghei.
    Annals of tropical medicine and parasitology, 1982, Volume: 76, Issue:1

    Topics: Animals; Antimalarials; Drug Resistance; Malaria; Male; Mice; Plasmodium berghei; Pyrimethamine; Triazines

1982
Analysis in yeast of antimalaria drugs that target the dihydrofolate reductase of Plasmodium falciparum.
    Molecular and biochemical parasitology, 1997, Volume: 85, Issue:1

    Topics: Animals; Antimalarials; Chloroquine; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Phenanthrenes; Plasmodium falciparum; Pyrimethamine; Recombinant Proteins; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines

1997
Plasmodium falciparum: kinetic interactions of WR99210 with pyrimethamine-sensitive and pyrimethamine-resistant dihydrofolate reductase.
    Experimental parasitology, 1997, Volume: 87, Issue:3

    Topics: Animals; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance; Folic Acid Antagonists; Kinetics; Plasmodium falciparum; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

1997
Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples.
    The American journal of tropical medicine and hygiene, 1999, Volume: 61, Issue:1

    Topics: Alleles; Animals; Antimalarials; DNA Primers; DNA Restriction Enzymes; DNA, Protozoan; Humans; Inhibitory Concentration 50; Kenya; Malaria, Falciparum; Plasmodium falciparum; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines

1999
The selectable marker human dihydrofolate reductase enables sequential genetic manipulation of the Plasmodium berghei genome.
    Molecular and biochemical parasitology, 2000, Mar-05, Volume: 106, Issue:2

    Topics: Animals; Animals, Genetically Modified; Antimalarials; Base Sequence; DNA Primers; Drug Resistance; Folic Acid Antagonists; Genetic Markers; Genome, Protozoan; Humans; Plasmids; Plasmodium berghei; Protozoan Proteins; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Transfection; Triazines

2000
Interaction of pyrimethamine, cycloguanil, WR99210 and their analogues with Plasmodium falciparum dihydrofolate reductase: structural basis of antifolate resistance.
    Bioorganic & medicinal chemistry, 2000, Volume: 8, Issue:5

    Topics: Amino Acid Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Molecular Structure; Proguanil; Pyrimethamine; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2000
Novel alleles of the Plasmodium falciparum dhfr highly resistant to pyrimethamine and chlorcycloguanil, but not WR99210.
    Molecular and biochemical parasitology, 2001, Sep-28, Volume: 117, Issue:1

    Topics: Alleles; Amino Acid Substitution; Animals; Antimalarials; Drug Resistance; Genes, Protozoan; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Protein Conformation; Pyrimethamine; Saccharomyces cerevisiae; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Triazines

2001
Molecular modeling of wild-type and antifolate resistant mutant Plasmodium falciparum DHFR.
    Biophysical chemistry, 2002, Aug-02, Volume: 98, Issue:3

    Topics: Animals; Chickens; Drug Resistance; Folic Acid Antagonists; Humans; Liver; Malaria, Falciparum; Models, Chemical; Models, Genetic; Models, Molecular; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Sequence Alignment; Tetrahydrofolate Dehydrogenase; Triazines

2002
Development of a yeast assay for rapid screening of inhibitors of human-derived Pneumocystis carinii dihydrofolate reductase.
    Antimicrobial agents and chemotherapy, 2002, Volume: 46, Issue:9

    Topics: Animals; Drug Evaluation, Preclinical; Folic Acid Antagonists; Humans; Pneumocystis; Pneumocystis Infections; Pyrimethamine; Rats; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim; Trimetrexate

2002
Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax.
    Proceedings of the National Academy of Sciences of the United States of America, 2002, Oct-01, Volume: 99, Issue:20

    Topics: Alleles; Amino Acid Sequence; Animals; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance; Inhibitory Concentration 50; Malaria; Molecular Sequence Data; Mutagenesis, Site-Directed; Mutation; Plasmids; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Recombinant Proteins; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2002
An amino acid substitution in the Babesia bovis dihydrofolate reductase-thymidylate synthase gene is correlated to cross-resistance against pyrimethamine and WR99210.
    Molecular and biochemical parasitology, 2004, Volume: 133, Issue:2

    Topics: Amino Acid Sequence; Amino Acid Substitution; Animals; Antiprotozoal Agents; Babesia bovis; Binding Sites; DNA, Protozoan; Drug Resistance; Exons; Folic Acid Antagonists; Gene Order; Genes, Protozoan; Models, Molecular; Molecular Sequence Data; Multienzyme Complexes; Mutation; Pyrimethamine; Sequence Alignment; Sequence Analysis, DNA; Sequence Homology, Amino Acid; Synteny; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

2004
Translational up-regulation of antifolate drug targets in the human malaria parasite Plasmodium falciparum upon challenge with inhibitors.
    Molecular and biochemical parasitology, 2004, Volume: 136, Issue:1

    Topics: Animals; Enzyme Inhibitors; Fluorouracil; Folic Acid Antagonists; Plasmodium falciparum; Protein Biosynthesis; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines; Up-Regulation

2004
Novel alleles of Plasmodium falciparum dhfr that confer resistance to chlorcycloguanil.
    Molecular and biochemical parasitology, 2005, Volume: 139, Issue:1

    Topics: Alleles; Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Mutagenesis, Site-Directed; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2005
Amino acid mutations in Plasmodium vivax DHFR and DHPS from several geographical regions and susceptibility to antifolate drugs.
    The American journal of tropical medicine and hygiene, 2006, Volume: 75, Issue:4

    Topics: Amino Acid Sequence; Animals; Antimalarials; Asia, Southeastern; China; Dihydropteroate Synthase; Drug Combinations; Drug Resistance; Folic Acid Antagonists; Humans; Melanesia; Molecular Sequence Data; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines

2006
The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase.
    International journal for parasitology, 2007, Volume: 37, Issue:7

    Topics: Animals; Catalysis; DNA, Protozoan; Enzyme Stability; Escherichia coli; Folic Acid Antagonists; Genetic Complementation Test; Kinetics; Mutagenesis, Insertional; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Tryptophan

2007
High-efficiency transfection and drug selection of genetically transformed blood stages of the rodent malaria parasite Plasmodium berghei.
    Nature protocols, 2006, Volume: 1, Issue:1

    Topics: Animals; Antimalarials; Culture Techniques; Drug Resistance; Genetic Markers; Humans; Mice; Mutation; Plasmodium berghei; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Transfection; Transformation, Genetic; Triazines

2006
Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.
    PloS one, 2012, Volume: 7, Issue:7

    Topics: Amino Acid Substitution; Antimalarials; Cells, Cultured; Drug Resistance; Erythrocytes; Folic Acid Antagonists; Gene Dosage; Humans; Inhibitory Concentration 50; Mutagenesis, Insertional; Plasmodium falciparum; Plasmodium vivax; Proguanil; Protozoan Proteins; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection; Triazines

2012