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Literature summary extracted from

  • Cody, V.; Pace, J.; Queener, S.; Adair, O.; Gangjee, A.
    Kinetic and structural analysis for potent antifolate inhibition of Pneumocystis jirovecii, Pneumocystis carinii, and human dihydrofolate reductases and their active-site variants (2013), Antimicrob. Agents Chemother., 57, 2669-2677 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli Rosetta Gami B (DE3) Homo sapiens
1.5.1.3 recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli Rosetta Gami B (DE3) Pneumocystis carinii
1.5.1.3 recombinant expression of His-tagged wild-type enzyme in Escherichia coli Rosetta Gami B (DE3) Pneumocystis jirovecii

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.5.1.3 purified recombinant detagged wild-type enzyme and mutant K37Q in complex with inhibitor 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine, hanging drop vapour diffusion method, mixing of 20.4 mg/ml protein in 20 mM MES, pH 6.0, 100 mM KCl with a 0:1 molar excess of NADPH and inhibitor, and with reservoir solution containing 100 mM K2HPO4, pH 6.9, 60-64% saturated (NH4)2SO4, and 3% (v/v) ethyl alcohol, 0.01 ml drops, 4°C, for mutant K37Q/F69N, 10.9 mg/ml protein in 10 mM MES, pH 6.0, and 100 mM KCl, is mixed with with a 0:1 molar excess of NADPH and inhibitor, and with a reservoir solution containing 33-36% PEG 2000, 50 mM MES, pH 6.0, and 100 mM KCl, 14°C, X-ray diffraction structure determination and analysis at 2.2 A resolution, modeling Pneumocystis carinii
1.5.1.3 purified recombinant detagged wild-type enzyme and mutants Q35K and Q35K/N64F in complex with inhibitor 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine, hanging drop vapour diffusion method, mixing of 6.6-9.8 mg/ml protein in 100 mM K2HPO4, pH 6.9, and 30% saturated (NH4)2SO4 with a 0:1 molar excess of NADPH and inhibitor, and with reservoir solution containing 100 mM K2HPO4, pH 6.9, 60-64% saturated (NH4)2SO4, and 3% v/v ethyl alcohol, 0.01 ml drops, 14°C X-ray diffraction structure determination and analysis at 2.2 A resolution, molecular replacement methods using the coordinates for human DHFR, PDB ID 1U72, modeling Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.5.1.3 F69F site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 F69N site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 F69S site-directed mutagenesis Pneumocystis carinii
1.5.1.3 K37Q site-directed mutagenesis, the mutant exhibits increased sensitivity for inhibition by 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine compared to the wild-type enzyme Pneumocystis carinii
1.5.1.3 K37Q/F69N site-directed mutagenesis, the mutant exhibits increased sensitivity for inhibition by 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine compared to the wild-type enzyme. Structure analysis of the mutant in complex with TMP, overview Pneumocystis carinii
1.5.1.3 K37Q/F69S site-directed mutagenesis Pneumocystis carinii
1.5.1.3 K37S site-directed mutagenesis Pneumocystis carinii
1.5.1.3 K37S/F69N site-directed mutagenesis Pneumocystis carinii
1.5.1.3 K37S/F69S site-directed mutagenesis Pneumocystis carinii
1.5.1.3 N64F site-directed mutagenesis, the mutant exhibits increased sensitivity for inhibition by 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine compared to the wild-type enzyme Homo sapiens
1.5.1.3 N64S site-directed mutagenesis Homo sapiens
1.5.1.3 Q35K site-directed mutagenesis Homo sapiens
1.5.1.3 Q35K/N64F site-directed mutagenesis Homo sapiens
1.5.1.3 Q35K/N64S site-directed mutagenesis Homo sapiens
1.5.1.3 Q35S site-directed mutagenesis Homo sapiens
1.5.1.3 Q35S/N64F site-directed mutagenesis Homo sapiens
1.5.1.3 Q35S/N64S site-directed mutagenesis Homo sapiens
1.5.1.3 S37K site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 S37K/S69F site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 S37K/S69N site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 S37Q/S69F site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 S37Q/S69N site-directed mutagenesis Pneumocystis jirovecii
1.5.1.3 S73Q site-directed mutagenesis Pneumocystis jirovecii

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine OAAG324, a potent inhibitor of dihydrofolate reductase, analysis of the enzyme-inhibitor structure of wild-type enzyme and mutants Homo sapiens
1.5.1.3 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine OAAG324, a potent inhibitor of dihydrofolate reductase Pneumocystis carinii
1.5.1.3 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine OAAG324, a potent inhibitor of dihydrofolate reductase Pneumocystis jirovecii
1.5.1.3 2,4-diamino-6-[(3',4',5'-trichloroanilino)methyl]pyrido[2,3-d]pyrimidine
-
 Homo sapiens
1.5.1.3 2,4-diamino-6-[(3',4',5'-trichloroanilino)methyl]pyrido[2,3-d]pyrimidine
-
 Pneumocystis carinii
1.5.1.3 2,4-diamino-6-[(3',4',5'-trichloroanilino)methyl]pyrido[2,3-d]pyrimidine
-
 Pneumocystis jirovecii
1.5.1.3 dihydrofolic acid
-
 Pneumocystis carinii
1.5.1.3 methotrexate
-
 Homo sapiens
1.5.1.3 methotrexate
-
 Pneumocystis carinii
1.5.1.3 methotrexate
-
 Pneumocystis jirovecii
1.5.1.3 TMP structure and ligand binding conformation of TMP Homo sapiens
1.5.1.3 TMP structure and ligand binding conformation of TMP Pneumocystis carinii
1.5.1.3 TMP structure and ligand binding conformation of TMP Pneumocystis jirovecii
1.5.1.3 trimethoprim
-
 Homo sapiens
1.5.1.3 trimethoprim
-
 Pneumocystis carinii
1.5.1.3 trimethoprim
-
 Pneumocystis jirovecii

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.5.1.3 additional information
-
 additional information Michaelis-Menten steady-state kinetics Homo sapiens
1.5.1.3 additional information
-
 additional information Michaelis-Menten steady-state kinetics Pneumocystis carinii
1.5.1.3 additional information
-
 additional information Michaelis-Menten steady-state kinetics Pneumocystis jirovecii
1.5.1.3 0.0004
-
 7,8-dihydrofolate recombinant mutant Q35K/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0004
-
 7,8-dihydrofolate recombinant mutant Q35S/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0005
-
 7,8-dihydrofolate recombinant mutant Q35K, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0007
-
 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0007
-
 7,8-dihydrofolate recombinant mutant Q35K/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0007
-
 7,8-dihydrofolate recombinant mutant Q35S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0007
-
 7,8-dihydrofolate recombinant mutant Q35S/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0008
-
 7,8-dihydrofolate recombinant mutant N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0009
-
 7,8-dihydrofolate recombinant mutant N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.002
-
 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0024
-
 7,8-dihydrofolate recombinant mutant S37K/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.003
-
 7,8-dihydrofolate recombinant mutant S37Q/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0032
-
 7,8-dihydrofolate recombinant mutant S37K/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0034
-
 7,8-dihydrofolate recombinant mutant S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0035
-
 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0035
-
 7,8-dihydrofolate recombinant mutant S37Q, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0038
-
 NADPH recombinant mutant Q35S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0038
-
 7,8-dihydrofolate recombinant mutant S37Q/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0045
-
 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0048
-
 7,8-dihydrofolate recombinant mutant S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0053
-
 NADPH recombinant mutant Q35S/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0056
-
 NADPH recombinant mutant Q35S/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0057
-
 NADPH recombinant mutant Q35K/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0063
-
 NADPH recombinant mutant N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0066
-
 7,8-dihydrofolate recombinant mutant F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0066
-
 NADPH recombinant mutant K37S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0066
-
 NADPH recombinant mutant Q35K/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.007
-
 NADPH recombinant mutant K37S/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0071
-
 7,8-dihydrofolate recombinant mutant F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0072
-
 NADPH recombinant mutant K37Q, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0075
-
 NADPH recombinant mutant N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0097
-
 7,8-dihydrofolate recombinant mutant K37S/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0101
-
 7,8-dihydrofolate recombinant mutant K37S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0106
-
 NADPH recombinant mutant K37Q/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0107
-
 7,8-dihydrofolate recombinant mutant K37Q/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0116
-
 7,8-dihydrofolate recombinant mutant K37S/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0118
-
 NADPH recombinant mutant S37Q, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0125
-
 NADPH recombinant mutant Q35K, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.0149
-
 NADPH recombinant mutant S37K/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0162
-
 NADPH recombinant mutant S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0163
-
 NADPH recombinant mutant F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0163
-
 NADPH recombinant mutant K37Q/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0167
-
 NADPH recombinant mutant K37S/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0173
-
 NADPH recombinant mutant S37Q/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0185
-
 7,8-dihydrofolate recombinant mutant K37Q/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0189
-
 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0192
-
 NADPH recombinant mutant F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.023
-
 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0252
-
 NADPH recombinant mutant S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0275
-
 NADPH recombinant mutant S37Q/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0864
-
 NADPH recombinant mutant S37K/S69N, pH 7.4, 37°C Pneumocystis jirovecii

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Homo sapiens
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 r
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Pneumocystis carinii
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 r
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Pneumocystis jirovecii
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Homo sapiens P00374
-
-
1.5.1.3 Pneumocystis carinii P16184
-
-
1.5.1.3 Pneumocystis jirovecii Q9UUP5
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.5.1.3 recombinant His-tagged wild-type and mutant enzymes from Escherichia coli Rosetta Gami B (DE3) by nickel affinity chromatography, and tag cleavage through the SUMO protease Ulp1, followed by another step of nickel affinity chromatography to remove the tag Homo sapiens
1.5.1.3 recombinant His-tagged wild-type and mutant enzymes from Escherichia coli Rosetta Gami B (DE3) by nickel affinity chromatography, and tag cleavage through the SUMO protease Ulp1, followed by another step of nickel affinity chromatography to remove the tag Pneumocystis carinii
1.5.1.3 recombinant His-tagged wild-type enzyme from Escherichia coli Rosetta Gami B (DE3) by nickel affinity chromatography, and tag cleavage through the SUMO protease Ulp1, followed by another step of nickel affinity chromatography to remove the tag Pneumocystis jirovecii

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Homo sapiens 5,6,7,8-tetrahydrofolate + NADP+
-
 r
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Pneumocystis carinii 5,6,7,8-tetrahydrofolate + NADP+
-
 r
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Pneumocystis jirovecii 5,6,7,8-tetrahydrofolate + NADP+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 DHFR
-
 Homo sapiens
1.5.1.3 DHFR
-
 Pneumocystis carinii
1.5.1.3 DHFR
-
 Pneumocystis jirovecii

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.5.1.3 37
-
 assay at Homo sapiens
1.5.1.3 37
-
 assay at Pneumocystis carinii
1.5.1.3 37
-
 assay at Pneumocystis jirovecii

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5.1.3 2 8 NADPH recombinant mutant N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 2 8 7,8-dihydrofolate recombinant mutant N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 3 6 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 3 6 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 3 6 NADPH recombinant mutant N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 3 6 7,8-dihydrofolate recombinant mutant N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 3 6 NADPH recombinant mutant Q35K/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 3 6 7,8-dihydrofolate recombinant mutant Q35K/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 21
-
 NADPH recombinant mutant Q35S/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 21
-
 7,8-dihydrofolate recombinant mutant Q35S/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 23
-
 NADPH recombinant mutant Q35S/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 23
-
 7,8-dihydrofolate recombinant mutant Q35S/N64S, pH 7.4, 37°C Homo sapiens
1.5.1.3 24
-
 NADPH recombinant mutant Q35S, pH 7.4, 37°C Homo sapiens
1.5.1.3 24
-
 7,8-dihydrofolate recombinant mutant Q35S, pH 7.4, 37°C Homo sapiens
1.5.1.3 26
-
 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Homo sapiens
1.5.1.3 26
-
 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Homo sapiens
1.5.1.3 26
-
 NADPH recombinant mutant S37Q/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 26
-
 7,8-dihydrofolate recombinant mutant S37Q/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 38
-
 NADPH recombinant mutant K37Q, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 38
-
 7,8-dihydrofolate recombinant mutant K37Q, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 39
-
 NADPH recombinant mutant Q35K, pH 7.4, 37°C Homo sapiens
1.5.1.3 39
-
 7,8-dihydrofolate recombinant mutant Q35K, pH 7.4, 37°C Homo sapiens
1.5.1.3 43
-
 NADPH recombinant mutant Q35K/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 43
-
 7,8-dihydrofolate recombinant mutant Q35K/N64F, pH 7.4, 37°C Homo sapiens
1.5.1.3 45
-
 NADPH recombinant mutant K37S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 45
-
 7,8-dihydrofolate recombinant mutant K37S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 47
-
 NADPH recombinant mutant S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 47
-
 7,8-dihydrofolate recombinant mutant S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 51
-
 NADPH recombinant mutant S37Q, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 51
-
 7,8-dihydrofolate recombinant mutant S37Q, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 57
-
 NADPH recombinant mutant S37K/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 57
-
 7,8-dihydrofolate recombinant mutant S37K/S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 78
-
 NADPH recombinant mutant S37K/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 78
-
 7,8-dihydrofolate recombinant mutant S37K/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 83
-
 NADPH recombinant mutant S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 83
-
 7,8-dihydrofolate recombinant mutant S69F, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 95
-
 NADPH recombinant mutant S37Q/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 95
-
 7,8-dihydrofolate recombinant mutant S37Q/S69N, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 157
-
 NADPH recombinant mutant K37S/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 157
-
 7,8-dihydrofolate recombinant mutant K37S/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 158
-
 NADPH recombinant mutant K37Q/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 158
-
 7,8-dihydrofolate recombinant mutant K37Q/F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 190
-
 NADPH recombinant mutant K37S/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 190
-
 7,8-dihydrofolate recombinant mutant K37S/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 204
-
 NADPH recombinant mutant F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 204
-
 7,8-dihydrofolate recombinant mutant F69S, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 223
-
 NADPH recombinant mutant K37Q/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 223
-
 7,8-dihydrofolate recombinant mutant K37Q/F69N, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 235
-
 NADPH recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 235
-
 7,8-dihydrofolate recombinant wild-type enzyme, pH 7.4, 37°C Pneumocystis carinii

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.5.1.3 7.4
-
 assay at Homo sapiens
1.5.1.3 7.4
-
 assay at Pneumocystis carinii
1.5.1.3 7.4
-
 assay at Pneumocystis jirovecii

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADP+
-
 Homo sapiens
1.5.1.3 NADP+
-
 Pneumocystis carinii
1.5.1.3 NADP+
-
 Pneumocystis jirovecii
1.5.1.3 NADPH
-
 Homo sapiens
1.5.1.3 NADPH
-
 Pneumocystis carinii
1.5.1.3 NADPH
-
 Pneumocystis jirovecii

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 additional information
-
 additional information inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis carinii, overview Pneumocystis jirovecii
1.5.1.3 additional information
-
 additional information inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Homo sapiens and Pneumocystis jirovecii, overview Pneumocystis carinii
1.5.1.3 additional information
-
 additional information inhibition kinetics of wild-type and mutant enzymes, comparison with the inhibition kinetics of enzymes and enzyme mutants from Pneumocystis carinii and Pneumocystis jirovecii, overview Homo sapiens
1.5.1.3 0.00000026
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine mutant K37Q enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.00000058
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine recombinant mutant N64F enzyme, pH 7.4, 37°C Homo sapiens
1.5.1.3 0.00000071
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine mutant K37Q/F69N enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0000008
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine mutant K37S enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.00000142
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine mutant K37S/F69S enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0000027
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine wild-type enzyme, pH 7.4, 37°C Pneumocystis jirovecii
1.5.1.3 0.0000063
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine wild-type enzyme, pH 7.4, 37°C Pneumocystis carinii
1.5.1.3 0.0000244
-
 2,4-diamino-6-[(2',5'-dichloroanilino)methyl]pyrido[2,3-d]pyrimidine recombinant wild-type enzyme, pH 7.4, 37°C Homo sapiens

General Information

EC Number General Information Comment Organism
1.5.1.3 additional information homology model of enzyme pjDHFR in ternary complex with NADPH and inhibitor 2,4-diamino-6-[(2',5'-dichloro anilino)methyl]pyrido[2,3-d]pyrimidine Pneumocystis jirovecii