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Literature summary extracted from

  • Deng, X.; Gujjar, R.; El Mazouni, F.; Kaminsky, W.; Malmquist, N.A.; Goldsmith, E.J.; Rathod, P.K.; Phillips, M.A.
    Structural plasticity of malaria dihydroorotate dehydrogenase allows selective binding of diverse chemical scaffolds (2009), J. Biol. Chem., 284, 26999-27009.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.3.5.2 in complex with inhibitors 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, and 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine to 2.0 A, 2.4 A, and 2.5 A resolution, respectively Plasmodium falciparum

Protein Variants

EC Number Protein Variants Comment Organism
1.3.5.2 F188A mutation has minimal effect on catalytic efficiency. IC50 value for inhibitor 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine increases 30-50fold Plasmodium falciparum
1.3.5.2 F227A mutation has minimal effect on catalytic efficiency. IC50 value for inhibitor 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine increases 30-50fold Plasmodium falciparum
1.3.5.2 H185A mutation has minimal effect on catalytic efficiency. IC50 value for inhibitor 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine increases 30-50fold Plasmodium falciparum
1.3.5.2 R265A mutation has minimal effect on catalytic efficiency. IC50 value for inhibitor 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine increases 30-50fold Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.5.2 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine i.e. DSM1 Plasmodium falciparum
1.3.5.2 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine i.e. DSM74 Plasmodium falciparum
1.3.5.2 N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine i.e. DSM2 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
1.3.5.2 Plasmodium falciparum Q08210
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Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.5.2 dihydroorotate + coenzyme Q coenzyme OD possesses a decyl tail Plasmodium falciparum orotate + reduced coenzyme Q
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IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.5.2 0.00021
-
pH 8.0, 20°C, mutant F188A Plasmodium falciparum N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0013
-
pH 8.0, 20°C, mutant F227A Plasmodium falciparum 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0013
-
pH 8.0, 20°C, mutant H185A Plasmodium falciparum 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0013
-
pH 8.0, 20°C, mutant H185A Plasmodium falciparum N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0014
-
pH 8.0, 20°C, mutant F188A Plasmodium falciparum 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0021
-
pH 8.0, 20°C, mutant F188A Plasmodium falciparum 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0021
-
pH 8.0, 20°C, mutant R265A Plasmodium falciparum 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0024
-
pH 8.0, 20°C, mutant R265A Plasmodium falciparum N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0044
-
pH 8.0, 20°C, mutant F227A Plasmodium falciparum N-anthracen-2-yl-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0063
-
pH 8.0, 20°C, mutant F227A Plasmodium falciparum 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.023
-
pH 8.0, 20°C, mutant R265A Plasmodium falciparum 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.025
-
pH 8.0, 20°C, mutant H185A Plasmodium falciparum 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine