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Literature summary extracted from

  • Kumar, P.; Kumar, A.; Verma, S.S.; Dwivedi, N.; Singh, N.; Siddiqi, M.I.; Tripathi, R.P.; Dube, A.; Singh, N.
    Leishmania donovani pteridine reductase 1: biochemical properties and structure-modeling studies (2008), Exp. Parasitol., 120, 73-79.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.5.1.33 drug development target for antifolate chemotherapy against Leishmania Leishmania donovani

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.5.1.33 expression of GFP-tagged enzyme in Leishmania donovani Leishmania donovani

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.33 (4-fluoro-phenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid ethyl ester
-
 Leishmania donovani
1.5.1.33 2,6-dimethyl [3-O-benzyl-1,2-O isopropylidene-beta-L-threo-pentofuronose-4-yl]-1-phenyl-1,4-dihydro pyridine-3,5-dicarboxylic acid diethyl ether
-
 Leishmania donovani
1.5.1.33 sodium antimony gluconate
-
 Leishmania donovani

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.5.1.33 2 biopterin + 3 NADPH + 3 H+ Leishmania donovani salvage of pterins, enzyme acts as a metabolic bypass for drugs targeting dihydrofolate reductase, PTR1 contributes about 10% of the reduction of folates in wild-type cells while the remaining 90% is due to the activity of dihydrofolate reductase-thymidylate synthase (EC 1.5.1.3) dihydrobiopterin + tetrahydrobiopterin + 3 NADP+
-
 ?
1.5.1.33 folate + NADPH + H+ Leishmania donovani
-
 7,8-dihydrofolate + tetrahydrofolate + NADP+
-
 ?

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.33 2 biopterin + 3 NADPH + 3 H+ salvage of pterins, enzyme acts as a metabolic bypass for drugs targeting dihydrofolate reductase, PTR1 contributes about 10% of the reduction of folates in wild-type cells while the remaining 90% is due to the activity of dihydrofolate reductase-thymidylate synthase (EC 1.5.1.3) Leishmania donovani dihydrobiopterin + tetrahydrobiopterin + 3 NADP+
-
 ?
1.5.1.33 folate + NADPH + H+
-
 Leishmania donovani 7,8-dihydrofolate + tetrahydrofolate + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.5.1.33 pteridine reductase 1
-
 Leishmania donovani
1.5.1.33 PTR1
-
 Leishmania donovani

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.33 NADPH
-
 Leishmania donovani

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.33 12.1
-
 amastigote Leishmania donovani sodium antimony gluconate
1.5.1.33 18.3
-
 amastigote Leishmania donovani 2,6-dimethyl [3-O-benzyl-1,2-O isopropylidene-beta-L-threo-pentofuronose-4-yl]-1-phenyl-1,4-dihydro pyridine-3,5-dicarboxylic acid diethyl ether
1.5.1.33 23.1
-
 amastigote Leishmania donovani (4-fluoro-phenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid ethyl ester
1.5.1.33 90.8
-
 promastigote Leishmania donovani 2,6-dimethyl [3-O-benzyl-1,2-O isopropylidene-beta-L-threo-pentofuronose-4-yl]-1-phenyl-1,4-dihydro pyridine-3,5-dicarboxylic acid diethyl ether
1.5.1.33 101
-
 promastigote Leishmania donovani (4-fluoro-phenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid ethyl ester