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Literature summary extracted from

  • Saravanamuthu, A.; Vickers, T.J.; Bond, C.S.; Peterson, M.R.; Hunter, W.N.; Fairlamb, A.H.
    Two interacting binding sites for quinacrine derivatives in the active site of trypanothione reductase: a template for drug design (2004), J. Biol. Chem., 279, 29493-29500.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.8.1.12 pharmacology enzyme is a target for selective drug design Trypanosoma cruzi

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.8.1.12 purified recombinant enzyme, reduced by NADPH, inactivated by binding of quinacrine mustard, 13 mg/ml enzyme-inhibitor complex in Na+ malate, pH 6.0, with precipitant 20% w/v PEG 8000, X-ray diffraction structure determination and analysis at 2.7 A resolution Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 MelT adduct of melarsen oxide with dihydrotrypanothione Trypanosoma cruzi
1.8.1.12 Quinacrine competitive Trypanosoma cruzi
1.8.1.12 quinacrine mustard enzyme and inhibitor first forms a reversible complex, then irreversible inactivation of NADPH-reduced and oxidized enzyme occurs, enzyme contains 2 interacting binding sites in the active site for the inhibitors, 2 inhibitor molecules per enzyme monomer are bound, addition of 2-mercaptoethanol prevents inactivation up to 25 mM, clomipramine strongly protects th enzyme from inactivation Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.8.1.12 trypanothione disulfide + NADPH Trypanosoma cruzi kex enzyme in the tryanothione-based redox metabolism of pathogenic trypanosomes trypanothione + NADP+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 no activity in Homo sapiens
-
-
-
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
-
 Trypanosoma cruzi trypanothione + NADP+
-
 ?
1.8.1.12 trypanothione disulfide + NADPH kex enzyme in the tryanothione-based redox metabolism of pathogenic trypanosomes Trypanosoma cruzi trypanothione + NADP+
-
 ?

Subunits

EC Number Subunits Comment Organism
1.8.1.12 dimer
-
 Trypanosoma cruzi

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 trypanothione reductase
-
 Trypanosoma cruzi
1.8.1.12 TryR
-
 Trypanosoma cruzi

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.8.1.12 27
-
 assay at Trypanosoma cruzi

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.8.1.12 7.5
-
 assay at Trypanosoma cruzi

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 additional information enzyme is a flavoprotein Trypanosoma cruzi
1.8.1.12 NADPH
-
 Trypanosoma cruzi

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.8.1.12 additional information
-
 additional information inhibition kinetics Trypanosoma cruzi
1.8.1.12 0.012
-
 MelT pH 7.5, 27°C Trypanosoma cruzi