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Literature summary for 1.8.1.12 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

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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

Inhibitors Comment Organism Structure
MelT adduct of melarsen oxide with dihydrotrypanothione Trypanosoma cruzi
Quinacrine competitive Trypanosoma cruzi
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)

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

Organism

Organism UniProt Comment Textmining
no activity in Homo sapiens
-
-
-
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
dimer
-
Trypanosoma cruzi

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
Trypanosoma cruzi
TryR
-
Trypanosoma cruzi

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

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

Ki Value [mM]

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