Literature summary for 1.8.1.12 extracted from

Czechowicz, J.A.; Wilhelm, A.K.; Spalding, M.D.; Larson, A.M.; Engel, L.K.; Alberg, D.G.
The synthesis and inhibitory activity of dethiotrypanothione and analogues against trypanothione reductase (2007), J. Org. Chem., 72, 3689-3693.

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Application

Application	Comment	Organism
pharmacology	trypanothione reductase plays a central role in the trypanosomatid parasites defense against oxidative stress, trypanothione reductase is a promising target for antitrypanosomal drugs, synthesis of dethiotrypanothione and related trypanothione analogues featuring ring-closing olefin metathesis macrocyclizations is described	Trypanosoma cruzi

Inhibitors

Inhibitors	Comment	Organism	Structure
bis(9H-fluoren-9-ylmethyl) [(18S,23S)-3,14,17,24-tetraoxo-1,4,8,13,16-pentaazacyclotetracosane-18,23-diyl]biscarbamate	lack the disulfide and trypanothione's gamma-glutamyl groups have been replaced by hydrophobic aromatic moieties	Trypanosoma cruzi
dethiotrypanothione	trypanothione disulfide analogue 2, lack the disulfide	Trypanosoma cruzi
dibenzyl [(18S,23S)-3,14,17,24-tetraoxo-1,4,8,13,16-pentaazacyclotetracosane-18,23-diyl]biscarbamate	lack the disulfide and trypanothione's gamma-glutamyl groups have been replaced by hydrophobic aromatic moieties	Trypanosoma cruzi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 + H+	-	Trypanosoma cruzi	trypanothione + NADP+	-	r

Synonyms

Synonyms	Comment	Organism
trypanothione reductase	TR	Trypanosoma cruzi
trypanothione-disulfide reductase	-	Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.016	-	bis(9H-fluoren-9-ylmethyl) [(18S,23S)-3,14,17,24-tetraoxo-1,4,8,13,16-pentaazacyclotetracosane-18,23-diyl]biscarbamate	-	Trypanosoma cruzi
0.145	-	dibenzyl [(18S,23S)-3,14,17,24-tetraoxo-1,4,8,13,16-pentaazacyclotetracosane-18,23-diyl]biscarbamate	-	Trypanosoma cruzi
0.826	-	dethiotrypanothione	-	Trypanosoma cruzi

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Release 2023.1 (January 2023)