Literature summary for 1.8.1.12 extracted from

Dixon, M.J.; Maurer, R.I.; Biggi, C.; Oyarzabal, J.; Essex, J.W.; Bradley, M.
Mechanism and structure-activity relationships of norspermidine-based peptidic inhibitors of trypanothione reductase (2005), Bioorg. Med. Chem., 13, 4513-4526.

Inhibitors

Inhibitors	Comment	Organism
N1,N9-bis-(L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide))-norspermidine	non-competitive inhibitor	Trypanosoma cruzi
N1,N9-bis-(L-tryptophanyl)-norspermidine	competitive inhibitor	Trypanosoma cruzi
N1,N9-bis-(L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide))-norspermidine	non-competitive inhibitor	Trypanosoma cruzi
N1,N9-bis-(L-tryptophanyl-L-arginyl)-norspermidine	non-competitive inhibitor	Trypanosoma cruzi
N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-acetyl-norspermidine	-	Trypanosoma cruzi
N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-L-arginyl-norspermidine	non-competitive inhibitor	Trypanosoma cruzi
N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	-	Trypanosoma cruzi
N1-L-arginyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
N1-L-arginyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
N1-L-arginyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-acetyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl-N9-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	non-competitive inhibitor	Trypanosoma cruzi
N1-L-tryptophanyl-L-arginyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
N1-L-tryptophanyl-norspermidine	-	Trypanosoma cruzi

Molecular Weight [Da]

Molecular Weight [Da]	Molecular Weight Maximum [Da]	Comment	Organism
103000	-	gel filtration	Trypanosoma cruzi

Organism

Organism	UniProt	Comment	Textmining
Trypanosoma cruzi	-	-	-

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
trypanothione reductase	-	Trypanosoma cruzi

Cofactor

Cofactor	Comment	Organism	Structure
NADPH	-	Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
0.00016	-	N1,N9-bis-(L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide))-norspermidine	-	Trypanosoma cruzi
0.00022	-	N1-L-tryptophanyl-L-arginyl-N9-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	-	Trypanosoma cruzi
0.003	-	N1,N9-bis-(L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide))-norspermidine	-	Trypanosoma cruzi
0.006	-	N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
0.007	-	N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
0.009	-	N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	-	Trypanosoma cruzi
0.011	-	N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-L-arginyl-norspermidine	-	Trypanosoma cruzi
0.012	-	N1-L-tryptophanyl-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-acetyl-norspermidine	-	Trypanosoma cruzi
0.014	-	N1,N9-bis-(L-tryptophanyl-L-arginyl)-norspermidine	-	Trypanosoma cruzi
0.019	-	N1,N9-bis-(L-tryptophanyl)-norspermidine	-	Trypanosoma cruzi
0.024	-	N1-L-tryptophanyl-L-arginyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
0.069	-	N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-N9-acetyl-norspermidine	-	Trypanosoma cruzi
0.069	-	N1-L-tryptophanyl-L-arginyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
0.083	-	N1-L-tryptophanyl-L-arginyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-tryptophanyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-tryptophanyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-tryptophanyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-arginyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-arginyl-N9-acetyl-norspermidine	-	Trypanosoma cruzi
0.1	-	N1-L-arginyl-N9-hexanoyl-norspermidine	-	Trypanosoma cruzi
0.131	-	N1-L-arginyl(2,2,5,7,8-pentamethylchroman-6-sulfonamide)-norspermidine	-	Trypanosoma cruzi