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Literature summary for 1.8.1.12 extracted from

  • Baiocco, P.; Poce, G.; Alfonso, S.; Cocozza, M.; Porretta, G.C.; Colotti, G.; Biava, M.; Moraca, F.; Botta, M.; Yardley, V.; Fiorillo, A.; Lantella, A.; Malatesta, F.; Ilari, A.
    Inhibition of Leishmania infantum trypanothione reductase by azole-based compounds: a comparative analysis with its physiological substrate by X-ray crystallography (2013), ChemMedChem, 8, 1175-1183.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Leishmania infantum

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Leishmania infantum

Inhibitors

Inhibitors Comment Organism Structure
4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine most active inhibitor Leishmania infantum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.023
-
trypanothione disulfide in the absence of 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
0.053
-
trypanothione disulfide in the presence of 0.01 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
0.075
-
trypanothione disulfide in the presence of 0.03 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
trypanothione disulfide + NADPH + H+ Leishmania infantum
-
trypanothione + NADP+
-
ir

Organism

Organism UniProt Comment Textmining
Leishmania infantum A4HSF7
-
-

Purification (Commentary)

Purification (Comment) Organism
in complex with inhibitor 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine Leishmania infantum

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
Leishmania infantum
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione disulfide + NADPH + H+
-
Leishmania infantum trypanothione + NADP+
-
ir

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
Leishmania infantum

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
11.4
-
trypanothione disulfide in the absence of 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
18
-
trypanothione disulfide in the presence of 0.01 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
19
-
trypanothione disulfide in the presence of 0.03 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum

Cofactor

Cofactor Comment Organism Structure
FAD
-
Leishmania infantum
NADPH
-
Leishmania infantum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0046
-
4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine at 20°C, pH not specified in the publication Leishmania infantum

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
250
-
trypanothione disulfide in the presence of 0.03 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
340
-
trypanothione disulfide in the presence of 0.01 mM 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum
470
-
trypanothione disulfide in the absence of 4-((1-(4-ethylphenyl)-2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-3-yl)methyl)thiomorpholine, at 20°C, pH not specified in the publication Leishmania infantum