Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Kao, T.T.; Wang, K.C.; Chang, W.N.; Lin, C.Y.; Chen, B.H.; Wu, H.L.; Shi, G.Y.; Tsai, J.N.; Fu, T.F.
    Characterization and comparative studies of zebrafish and human recombinant dihydrofolate reductases-inhibition by folic acid and polyphenols (2008), Drug Metab. Dispos., 36, 508-516.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.5.1.3 drug development comparison of Danio rerio and human enzyme to evaluate the suitability of the fish enzyme as an assay system for antifolate drug discovery. Structural and kinetic proterties of both enzymes are similar and susceptibilites to known inhibitors are also comparable Homo sapiens
1.5.1.3 drug development comparison of Danio rerio and human enzyme to evaluate the suitability of the fish enzyme as an assay system for antifolate drug discovery. Structural and kinetic proterties of both enzymes are similar and susceptibilities to known inhibitors are also comparable Danio rerio

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.3 expression in Escherichia coli Homo sapiens
1.5.1.3 expression in Escherichia coli Danio rerio

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 epigallocatechin-3-gallate IC50 value around 0.1 mM Danio rerio
1.5.1.3 epigallocatechin-3-gallate IC50 value around 0.1 mM Homo sapiens
1.5.1.3 folate substrate inhibition, IC50 value around 0.02 mM Danio rerio
1.5.1.3 folate substrate inhibition, IC50 value around 0.02 mM Homo sapiens
1.5.1.3 methotrexate 60 nM, complete inhibition Danio rerio
1.5.1.3 methotrexate 60 nM, complete inhibition Homo sapiens
1.5.1.3 trimethoprim IC50 value around 0.01 mM Danio rerio
1.5.1.3 trimethoprim IC50 value around 0.07 mM Homo sapiens

Organic Solvent Stability

EC Number Organic Solvent Comment Organism
1.5.1.3 dimethyl sulfoxide less than 3% inhibition in presence of dimethylsulfoxide at concentrations used for inhibitor dissolvation Homo sapiens
1.5.1.3 dimethyl sulfoxide less than 3% inhibition in presence of dimethylsulfoxide at concentrations used for inhibitor dissolvation Danio rerio

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Danio rerio Q6IQS4
-
-
1.5.1.3 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.5.1.3 recombinant enzyme Homo sapiens
1.5.1.3 recombinant enzyme Danio rerio

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.5.1.3 brain highest level of enzyme present in ova and brain Danio rerio
-
1.5.1.3 embryo abundant expression at early stage, with an abrupt decrease after 3 days postfertilization Danio rerio
-
1.5.1.3 ovum highest level of enzyme present in ova and brain Danio rerio
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.5.1.3 6
-
 pH 7.0, 25°C Homo sapiens
1.5.1.3 13
-
 pH 7.0, 25°C, recombinant His-tagged enzyme Danio rerio

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+
-
 ?
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Danio rerio 5,6,7,8-tetrahydrofolate + NADP+
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.3 additional information
-
 folate, IC50 value around 0.02 mM, epigallocatechin-3-gallate, IC50 value around 0.1 mM, respectively Homo sapiens additional information
1.5.1.3 additional information
-
 folate, IC50 value around 0.02 mM, epigallocatechin-3-gallate, IC50 value around 0.1 mM, respectively Danio rerio additional information