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Literature summary 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)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.33 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

EC Number Organism UniProt Comment Textmining
1.5.1.33 Leishmania donovani
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.5.1.33 LdPTR1
-
 Leishmania donovani
1.5.1.33 pteridine reductase 1
-
 Leishmania donovani

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.33 NADPH
-
 Leishmania donovani

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.33 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

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.33 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