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Literature summary extracted from

  • Phillips, M.A.; Rathod, P.K.
    Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy (2010), Infect. Disord. Drug Targets, 10, 226-239.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
1.3.5.2 additional information activity of the bc1 complex is essential for providing oxidized ubiqinone to DHODH for the formation of pyrimidines Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.5.2 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
-
Homo sapiens
1.3.5.2 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
-
Plasmodium falciparum
1.3.5.2 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
-
Homo sapiens
1.3.5.2 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
-
Plasmodium falciparum
1.3.5.2 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
Homo sapiens
1.3.5.2 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
-
Plasmodium falciparum
1.3.5.2 5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
-
Homo sapiens
1.3.5.2 5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
-
Plasmodium falciparum
1.3.5.2 5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
-
Homo sapiens
1.3.5.2 5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
-
Plasmodium falciparum
1.3.5.2 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 6-methyl-N-phenyl-3aH-inden-4-amine
-
Homo sapiens
1.3.5.2 6-methyl-N-phenyl-3aH-inden-4-amine
-
Plasmodium falciparum
1.3.5.2 diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
-
Homo sapiens
1.3.5.2 diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
-
Plasmodium falciparum
1.3.5.2 ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
Homo sapiens
1.3.5.2 ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
-
Plasmodium falciparum
1.3.5.2 additional information screening for potent inhibitors of PfDHODH and effect on the human enzyme, overview. The compiunds show strong selectivity for the malarial enzyme over that from the human host, inhibition mechanism, overview Homo sapiens
1.3.5.2 additional information screening for potent inhibitors of PfDHODH that show strong selectivity for the malarial enzyme over that from the human host. Lead optimization of a triazolopyrimidine-based series, inhibition mechanism, overview Plasmodium falciparum
1.3.5.2 N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
-
Homo sapiens
1.3.5.2 N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
Homo sapiens
1.3.5.2 N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
Plasmodium falciparum
1.3.5.2 N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum
1.3.5.2 N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
-
Homo sapiens
1.3.5.2 N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
-
Plasmodium falciparum
1.3.5.2 N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Homo sapiens
1.3.5.2 N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
Plasmodium falciparum

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.3.5.2 mitochondrion a class 2 mitochondrial enzyme Homo sapiens 5739
-
1.3.5.2 mitochondrion a class 2 mitochondrial enzyme Plasmodium falciparum 5739
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.3.5.2 L-dihydroorotate + FMN Homo sapiens
-
orotate + FMNH2
-
?
1.3.5.2 L-dihydroorotate + FMN Plasmodium falciparum
-
orotate + FMNH2
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.3.5.2 Homo sapiens
-
-
-
1.3.5.2 Plasmodium falciparum Q08210
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.5.2 L-dihydroorotate + FMN
-
Homo sapiens orotate + FMNH2
-
?
1.3.5.2 L-dihydroorotate + FMN
-
Plasmodium falciparum orotate + FMNH2
-
?
1.3.5.2 L-dihydroorotate + FMN DHODH catalyzes the FMN-dependent oxidation of dihydroorotate to produce orotic acid. Two separate half reactions are required to complete the catalytic cycle: 1. oxidation of dihydroorotate driven by the reduction of FMN and, 2. reoxidation of FMNH2 to regenerate the active enzyme Homo sapiens orotate + FMNH2
-
?
1.3.5.2 L-dihydroorotate + FMN DHODH catalyzes the FMN-dependent oxidation of dihydroorotate to produce orotic acid. Two separate half reactions are required to complete the catalytic cycle: 1. oxidation of dihydroorotate driven by the reduction of FMN and, 2. reoxidation of FMNH2 to regenerate the active enzyme Plasmodium falciparum orotate + FMNH2
-
?

Synonyms

EC Number Synonyms Comment Organism
1.3.5.2 DHODH
-
Homo sapiens
1.3.5.2 DHODH
-
Plasmodium falciparum

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.5.2 FMN class 2 mitochondrial enzyme Homo sapiens
1.3.5.2 FMN class 2 mitochondrial enzyme Plasmodium falciparum
1.3.5.2 ubiquinone the mitochondrial enzyme requires oxidized ubiquinone, CoQ Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.5.2 0.000016
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
1.3.5.2 0.000042
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.000047
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00005
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
1.3.5.2 0.000056
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.000077
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.000083
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
1.3.5.2 0.00016
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
1.3.5.2 0.00016
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00017
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.00019
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00021
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00023
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
1.3.5.2 0.00028
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00029
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00034
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
1.3.5.2 0.00046
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.00047
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.0005
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00063
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.00068
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0007
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0007
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.00071
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.00078
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.00093
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
1.3.5.2 0.0014
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0017
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine
1.3.5.2 0.003
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.0092
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.01
-
above, pH not specified in the publication, temperature not specified in the publication Homo sapiens N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
1.3.5.2 0.01
-
above, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.01
-
above, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.019
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.03
-
pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide
1.3.5.2 0.05
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(2,4-dichlorophenyl)naphthalene-2-carboxamide
1.3.5.2 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 6-methyl-N-phenyl-3aH-inden-4-amine
1.3.5.2 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine
1.3.5.2 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.1
-
above, pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.11
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea
1.3.5.2 0.2
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
1.3.5.2 0.2
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide

General Information

EC Number General Information Comment Organism
1.3.5.2 physiological function the enzyme is involved in de novo biosynthesis of pyrimidines Homo sapiens
1.3.5.2 physiological function the enzyme is involved in de novo biosynthesis of pyrimidines, which is essential in malaria. Absence of pyrimidine salvage pathways in Plasmodium, thus the de novo pathway provides the only source of pyrimidines for cell growth. The mitochondrial enzyme requires oxidized ubiquinone, thus coupling pyrimidine biosynthesis to the respiratory chain Plasmodium falciparum