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Literature summary for 1.3.5.2 extracted from
- Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy (2010), Infect. Disord. Drug Targets, 10, 226-239.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | activity of the bc1 complex is essential for providing oxidized ubiqinone to DHODH for the formation of pyrimidines | Plasmodium falciparum |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea | - |
Homo sapiens |  |
| 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea | - |
Plasmodium falciparum | |
| 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol | - |
Homo sapiens | |
| 2-[(E)-2-(2-methylphenyl)ethenyl]quinolin-4-ol | - |
Plasmodium falciparum | |
| 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one | - |
Homo sapiens | |
| 4-pentyl-1,3,4,10-tetrahydroacridin-9(2H)-one | - |
Plasmodium falciparum | |
| 5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| 5,6-dimethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(1H-indol-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(2-methyl-1H-benzimidazol-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(2-methyl-1H-indol-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(4-methylpiperazin-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide | - |
Homo sapiens | |
| 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide | - |
Plasmodium falciparum | |
| 5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| 5-ethyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| 5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine | - |
Homo sapiens | |
| 5-methyl-7-(naphthalen-2-yloxy)[1,2,4]triazolo[1,5-a]pyrimidine | - |
Plasmodium falciparum | |
| 5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine | - |
Homo sapiens | |
| 5-methyl-7-(naphthalen-2-ylsulfanyl)[1,2,4]triazolo[1,5-a]pyrimidine | - |
Plasmodium falciparum | |
| 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| 5-methyl-N-(naphthalen-2-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| 5-methyl-N-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| 6-methyl-N-phenyl-3aH-inden-4-amine | - |
Homo sapiens | |
| 6-methyl-N-phenyl-3aH-inden-4-amine | - |
Plasmodium falciparum | |
| diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate | - |
Homo sapiens | |
| diethyl [(dibenzo[b,d]thiophen-2-ylamino)methylidene]propanedioate | - |
Plasmodium falciparum | |
| ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate | - |
Homo sapiens | |
| ethyl 4-(4-ethoxybenzyl)-3,5-dimethyl-1H-pyrrole-2-carboxylate | - |
Plasmodium falciparum | |
| 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 | |
| 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 | |
| N-(2,4-dichlorophenyl)naphthalene-2-carboxamide | - |
Homo sapiens | |
| N-(2,4-dichlorophenyl)naphthalene-2-carboxamide | - |
Plasmodium falciparum | |
| N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(2-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(2-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide | - |
Homo sapiens | |
| N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide | - |
Plasmodium falciparum | |
| N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(3-chlorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(3-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(4-bromophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(4-fluorophenyl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(anthracen-2-yl)-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-(anthracen-2-yl)-N,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
| N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide | - |
Homo sapiens | |
| N-propyl-5-(1H-pyrazol-1-yl)thiophene-2-carboxamide | - |
Plasmodium falciparum | |
| N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Homo sapiens | |
| N-[3-fluoro-4-(trifluoromethyl)phenyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | - |
Plasmodium falciparum | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| mitochondrion | a class 2 mitochondrial enzyme | Homo sapiens | 5739 | - |
| mitochondrion | a class 2 mitochondrial enzyme | Plasmodium falciparum | 5739 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-dihydroorotate + FMN | Homo sapiens | - |
orotate + FMNH2 | - |
? | |
| L-dihydroorotate + FMN | Plasmodium falciparum | - |
orotate + FMNH2 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Plasmodium falciparum | Q08210 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-dihydroorotate + FMN | - |
Homo sapiens | orotate + FMNH2 | - |
? | |
| L-dihydroorotate + FMN | - |
Plasmodium falciparum | orotate + FMNH2 | - |
? | |
| 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 | - |
? | |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| DHODH | - |
Homo sapiens |
| DHODH | - |
Plasmodium falciparum |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| FMN | class 2 mitochondrial enzyme | Homo sapiens | |
| FMN | class 2 mitochondrial enzyme | Plasmodium falciparum | |
| ubiquinone | the mitochondrial enzyme requires oxidized ubiquinone, CoQ | Plasmodium falciparum | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000016 | - |
pH not specified in the publication, temperature not specified in the publication | Plasmodium falciparum | N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide | |
| 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 | |
| 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 | |
| 0.00005 | - |
pH not specified in the publication, temperature not specified in the publication | Plasmodium falciparum | N-(2,4-dichlorophenyl)naphthalene-2-carboxamide | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 0.00023 | - |
pH not specified in the publication, temperature not specified in the publication | Plasmodium falciparum | 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 0.03 | - |
pH not specified in the publication, temperature not specified in the publication | Plasmodium falciparum | 5-(piperidin-1-yl)-N-propylthiophene-2-carboxamide | |
| 0.05 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(2,4-dichlorophenyl)naphthalene-2-carboxamide | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 0.11 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-(2-methoxyphenyl)-3-naphthalen-1-ylurea | |
| 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 | |
| 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
| General Information | Comment | Organism |
|---|---|---|
| physiological function | the enzyme is involved in de novo biosynthesis of pyrimidines | Homo sapiens |
| 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 |
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