Literature summary for 1.8.1.12 extracted from

Bonse, S.; Santelli-Rouvier, C.; Barbe, J.; Krauth-Siegel, R.L.
Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships (1999), J. Med. Chem., 42, 5448-5454.

Search for more literature for 1.8.1.12

Activating Compound

Activating Compound	Comment	Organism	Structure
additional information	activity is dependent on a redox-active cysteine at the active centre	Trypanosoma cruzi

Application

Application	Comment	Organism
medicine	potential target for drug design against trypanosomiasis	Trypanosoma cruzi

Inhibitors

Inhibitors	Comment	Organism	Structure
6-chlorotacrine	competitive inhibition	Trypanosoma cruzi
9-Amino-1,2,3,4-tetrahydroacridine	i.e. tacrine, competitive inhibition	Trypanosoma cruzi
9-aminoacridine derivatives	competitive inhibition	Trypanosoma cruzi
9-thioacridine derivatives	mixed-type inhibition	Trypanosoma cruzi
Mepacrine	i.e. quinacrine, competitive inhibition	Trypanosoma cruzi

Organism

Organism	UniProt	Comment	Textmining
Trypanosoma cruzi	-	-	-

Reaction

Reaction	Comment	Organism	Reaction ID
trypanothione + NADP+ = trypanothione disulfide + NADPH + H+	mechanistic reaction scheme, structure-function relation	Trypanosoma cruzi	a

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
trypanothione disulfide + NADPH	-	Trypanosoma cruzi	trypanothione + NADP+	-	?

Synonyms

Synonyms	Comment	Organism
TR	-	Trypanosoma cruzi

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Trypanosoma cruzi

Cofactor

Cofactor	Comment	Organism	Structure
FAD	-	Trypanosoma cruzi
NADPH	-	Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.007	0.043	9-aminoacridine derivatives	-	Trypanosoma cruzi
0.019	-	Mepacrine	-	Trypanosoma cruzi
0.021	0.037	9-thioacridine derivatives	-	Trypanosoma cruzi
0.08	-	6-chlorotacrine	-	Trypanosoma cruzi
0.14	-	9-Amino-1,2,3,4-tetrahydroacridine	-	Trypanosoma cruzi

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Release 2023.1 (January 2023)