Literature summary for 1.5.1.3 extracted from

Tobias, A.M.; Toska, D.; Lange, K.; Eck, T.; Bhat, R.; Janson, C.A.; Rotella, D.P.; Gubler, U.; Goodey, N.M.
Expression, purification, and inhibition profile of dihydrofolate reductase from the filarial nematode Wuchereria bancrofti (2018), PLoS ONE, 13, e0197173 .

Search for more literature for 1.5.1.3

Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli including 13 amino acid loop	Brugia malayi
expression in Escherichia coli including 13 amino acid loop	Wuchereria bancrofti

Inhibitors

Inhibitors	Comment	Organism	Structure
(-)-epicatechin	-	Brugia malayi
(-)-epicatechin	-	Wuchereria bancrofti
(-)-epicatechin gallate	-	Brugia malayi
(-)-epicatechin gallate	-	Wuchereria bancrofti
aminopterin	-	Brugia malayi
aminopterin	-	Wuchereria bancrofti
methotrexate	-	Brugia malayi
methotrexate	-	Wuchereria bancrofti
pyrimethamine	-	Brugia malayi
pyrimethamine	-	Wuchereria bancrofti
raltitrexed	-	Brugia malayi
raltitrexed	-	Wuchereria bancrofti
trimethoprim	-	Brugia malayi
trimethoprim	-	Wuchereria bancrofti
vitexin	-	Brugia malayi
vitexin	-	Wuchereria bancrofti

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0037	-	7,8-dihydrofolate	pH 6, 25°C	Wuchereria bancrofti
0.0147	-	7,8-dihydrofolate	pH 6, 25°C	Brugia malayi

Organism

Organism	UniProt	Comment	Textmining
Brugia malayi	-	-	-
Wuchereria bancrofti	J9F199	sequence lacks a crucial, conserved 13 amino acid loop	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant protein, using Ni-NTA resin and imidazole concentration in the wash buffer is changed from 25 mM to 100 mM	Brugia malayi
recombinant protein, using Ni-NTA resin and imidazole concentration in the wash buffer is changed from 25 mM to 100 mM	Wuchereria bancrofti

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
7,8-dihydrofolate + NADPH + H+	-	Brugia malayi	5,6,7,8-tetrahydrofolate + NADP+	-	?
7,8-dihydrofolate + NADPH + H+	-	Wuchereria bancrofti	5,6,7,8-tetrahydrofolate + NADP+	-	?

Synonyms

Synonyms	Comment	Organism
WUBG_00817	-	Wuchereria bancrofti

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
2.2	-	7,8-dihydrofolate	pH 6, 25°C	Brugia malayi
7.4	-	7,8-dihydrofolate	pH 6, 25°C	Wuchereria bancrofti

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000005	-	methotrexate	pH 6, 25°C	Brugia malayi
0.0000007	-	methotrexate	pH 6, 25°C	Wuchereria bancrofti
0.0000017	-	aminopterin	pH 6, 25°C	Brugia malayi
0.0000021	-	aminopterin	pH 6, 25°C	Wuchereria bancrofti
0.0016	-	raltitrexed	pH 6, 25°C	Brugia malayi
0.002	-	raltitrexed	pH 6, 25°C	Wuchereria bancrofti
0.0036	-	pyrimethamine	pH 6, 25°C	Brugia malayi
0.00598	-	trimethoprim	pH 6, 25°C	Wuchereria bancrofti
0.015	-	trimethoprim	pH 6, 25°C	Brugia malayi
0.015	-	pyrimethamine	pH 6, 25°C	Wuchereria bancrofti

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
additional information	-	value above 1 mM, pH 6, 25°C	Brugia malayi	(-)-epicatechin gallate
additional information	-	value above 1 mM, pH 6, 25°C	Wuchereria bancrofti	(-)-epicatechin gallate
additional information	-	value above 2.5 mM, pH 6, 25°C	Brugia malayi	(-)-epicatechin
additional information	-	value above 2.5 mM, pH 6, 25°C	Wuchereria bancrofti	(-)-epicatechin
0.0000022	-	pH 6, 25°C	Brugia malayi	methotrexate
0.0000075	-	pH 6, 25°C	Brugia malayi	aminopterin
0.000014	-	pH 6, 25°C	Wuchereria bancrofti	aminopterin
0.000018	-	pH 6, 25°C	Wuchereria bancrofti	methotrexate
0.0073	-	pH 6, 25°C	Brugia malayi	raltitrexed
0.016	-	pH 6, 25°C	Brugia malayi	pyrimethamine
0.018	-	pH 6, 25°C	Wuchereria bancrofti	raltitrexed
0.065	-	pH 6, 25°C	Brugia malayi	trimethoprim
0.083	-	pH 6, 25°C	Wuchereria bancrofti	trimethoprim
0.24	-	pH 6, 25°C	Brugia malayi	vitexin
0.24	-	pH 6, 25°C	Wuchereria bancrofti	vitexin
0.454	-	pH 6, 25°C	Wuchereria bancrofti	pyrimethamine

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Release 2023.1 (January 2023)