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Literature summary for 1.5.1.3 extracted from

  • Cody, V.; Chisum, K.; Pope, C.; Queener, S.F.
    Purification and characterization of human-derived Pneumocystis jirovecii dihydrofolate reductase expressed in Sf21 insect cells and in Escherichia coli (2005), Protein Expr. Purif., 40, 417-423.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
methotrexate 50% inhibition at 0.000000436 mM, recombinant rat-derived enzyme, 50% inhibition at 0.0000029 mM, recombinant human-derived enzyme Pneumocystis jirovecii
OAAG324 i.e. 6-([(2,5-dichlorophenyl)amino]methyl)pyrido[2,3-d]pyrimidine-2,4-diamine, 50% inhibition at 0.000262 mM, recombinant rat-derived enzyme, 50% inhibition at 0.0075 mM, recombinant human-derived enzyme Pneumocystis jirovecii
OAAG373 i.e. 6-([(3,4,5-trichlorophenyl)amino]methyl)pyrido[2,3-d]pyrimidine-2,4-diamine, 50% inhibition at 0.000139 mM, recombinant rat-derived enzyme, 50% inhibition at 0.00094 mM, recombinant human-derived enzyme Pneumocystis jirovecii
PY957 i.e. 5-(3-[(2,4-diaminopyrimidin-5-yl)methyl]-4-methoxyphenoxy)pentanoic acid, 50% inhibition at 0.00009833 mM, recombinant rat-derived enzyme Pneumocystis jirovecii
pyrimethamine 50% inhibition at 0.0024 mM, recombinant rat-derived enzyme, 50% inhibition at 0.0021 mM, recombinant human-derived enzyme Pneumocystis jirovecii
trimethoprim 50% inhibition at 0.027 mM, recombinant rat-derived enzyme, 50% inhibition at 0.0032 mM, recombinant human-derived enzyme Pneumocystis jirovecii

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.002
-
7,8-dihydrofolate His-tagged human-derived enzyme, pH 7.65 Pneumocystis jirovecii
0.0056
-
7,8-dihydrofolate recombinant rat-derived enzyme, pH 7.65 Pneumocystis jirovecii
0.0065
-
NADPH His-tagged human-derived enzyme, pH 7.65 Pneumocystis jirovecii
0.0106
-
7,8-dihydrofolate native rat-derived enzyme, pH 7.65 Pneumocystis jirovecii
0.0123
-
NADPH recombinant rat-derived enzyme, pH 7.65 Pneumocystis jirovecii
0.0167
-
NADPH native rat-derived enzyme, pH 7.65 Pneumocystis jirovecii

Organism

Organism UniProt Comment Textmining
Pneumocystis jirovecii
-
recombinant human-derived and rat-derived enzyme
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7,8-dihydrofolate + NADPH
-
Pneumocystis jirovecii 5,6,7,8-tetrahydrofolate + NADP+
-
?

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Pneumocystis jirovecii
NADPH
-
Pneumocystis jirovecii