Literature summary for 1.5.1.3 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.

Search for more literature for 1.5.1.3

Application

Application	Comment	Organism
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
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)

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

Inhibitors

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

Organic Solvent Stability

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

Organism

Organism	UniProt	Comment	Textmining
Danio rerio	Q6IQS4	-	-
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant enzyme	Homo sapiens
recombinant enzyme	Danio rerio

Source Tissue

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

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
7,8-dihydrofolate + NADPH + H+	-	Homo sapiens	5,6,7,8-tetrahydrofolate + NADP+	-	?
7,8-dihydrofolate + NADPH + H+	-	Danio rerio	5,6,7,8-tetrahydrofolate + NADP+	-	?

IC50 Value

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

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)