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Literature summary 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.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.8.1.12 pharmacology trypanothione reductase plays a central role in the trypanosomatid parasite’s 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

EC Number Inhibitors Comment Organism Structure
1.8.1.12 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lack the disulfide and trypanothione's gamma-glutamyl groups have been replaced by hydrophobic aromatic moieties Trypanosoma cruzi
1.8.1.12 dethiotrypanothione trypanothione disulfide analogue 2, lack the disulfide Trypanosoma cruzi
1.8.1.12 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lack the disulfide and trypanothione's gamma-glutamyl groups have been replaced by hydrophobic aromatic moieties Trypanosoma cruzi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

EC Number Organism UniProt Comment Textmining
1.8.1.12 Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.12 trypanothione disulfide + NADPH + H+
-
 Trypanosoma cruzi trypanothione + NADP+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 trypanothione reductase TR Trypanosoma cruzi
1.8.1.12 trypanothione-disulfide reductase
-
 Trypanosoma cruzi

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.8.1.12 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
1.8.1.12 0.145
-
 dibenzyl [(18S,23S)-3,14,17,24-tetraoxo-1,4,8,13,16-pentaazacyclotetracosane-18,23-diyl]biscarbamate
-
 Trypanosoma cruzi
1.8.1.12 0.826
-
 dethiotrypanothione
-
 Trypanosoma cruzi