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Literature summary for 1.5.1.33 extracted from

  • Kaur, J.; Sundar, S.; Singh, N.
    Molecular docking, structure-activity relationship and biological evaluation of the anticancer drug monastrol as a pteridine reductase inhibitor in a clinical isolate of Leishmania donovani (2010), J. Antimicrob. Chemother., 65, 1742-1748.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed as a His-tagged fusion protein Leishmania donovani

Inhibitors

Inhibitors Comment Organism Structure
4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-4H-pyrimidin-5-carboxylic acid ethyl ester both monastrol (R) and (S) enantiomers fit well in the ligand-binding pocket of LdPTR1. Monastrol is a potent inhibitor of PTR1 in Leishmania, it inhibits proliferation of amastigotes in macrophage cultures infected with an Leishmania donovani clinical isolate, with no host cytotoxicity Leishmania donovani

Organism

Organism UniProt Comment Textmining
Leishmania donovani
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using Ni-NTA chromatography Leishmania donovani

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
biopterin + 2 NADPH + 2 H+
-
Leishmania donovani 5,6,7,8-tetrahydrobiopterin + 2 NADP+
-
?

Synonyms

Synonyms Comment Organism
LdPTR1
-
Leishmania donovani
pteridine reductase 1
-
Leishmania donovani

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Leishmania donovani

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000428
-
4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-4H-pyrimidin-5-carboxylic acid ethyl ester pH 4.8, 30°C Leishmania donovani

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.01
-
pH 4.8, 30°C Leishmania donovani 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-4H-pyrimidin-5-carboxylic acid ethyl ester