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1.3.98.1: dihydroorotate dehydrogenase (fumarate)

This is an abbreviated version!
For detailed information about dihydroorotate dehydrogenase (fumarate), go to the full flat file.

Word Map on EC 1.3.98.1

Reaction

(S)-dihydroorotate
+
fumarate
=
Orotate
 +
succinate

Synonyms

(DHO) dehydrogenase, 4,5-L-dihydroorotate:oxygen oxidoreductase, ACT/DHOD, class 1A DHOD, class 1A DHODH, class 1A dihydroorotate dehydrogenase, DHOD, DHOD1, DHOD2, DHOD3, DHODA, DHOdehase, DHODH, DHODH-1A, dihydroorotate dehydrogenase, dihydroorotate dehydrogenase class 1A, Dihydroorotate oxidase, EC 1.3.3.1, LmDHODH, More, oxidase, dihydroorotate, TcDHOD

ECTree

     1 Oxidoreductases
         1.3 Acting on the CH-CH group of donors
             1.3.98 With other, known, physiological acceptors
                1.3.98.1 dihydroorotate dehydrogenase (fumarate)

Inhibitors

Inhibitors on EC 1.3.98.1 - dihydroorotate dehydrogenase (fumarate)

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,5-dihydrofuro[3,4-d]pyrimidine-2,4,7-trione
-
-
1-(1-naphthyl)-3-[2-(trifluoromethyl)phenyl]urea
-
50% inhibition at 0.0004 mM, wild type, 0.00034 mM, mutant R265A, above 0.2, mutant H185A
1-(2-methoxyphenyl)-3-(1-naphthyl)urea
-
50% inhibition at 0.00023 mM, wild type, 0.00024 mM, mutant R265A, 0.140, mutant H185A
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(4-methyl-benzylamide) 5-phenylamide
-
minimum inhibitory concentration 0.032 mg/ml
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-(isobutyl-amide)
-
minimum inhibitory concentration above 0.064 mg/ml
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[(4-carbamoyl-phenyl)-amide]
-
minimum inhibitory concentration 0.008 mg/ml
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide]
-
minimum inhibitory concentration 0.00025 mg/ml
1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[(4-piperidin-1-yl-phenyl)-amide] 3-[(pyridin-3-ylmethyl)-amide]
-
minimum inhibitory concentration 0.002 mg/ml
1-(4-chlorophenyl)-3-quinolin-8-ylurea
-
50% inhibition at 0.00078 mM, wild type, 0.002 mM, mutant R265A, above 0.4, mutant H185A
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(isobutyl-amide) 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
minimum inhibitory concentration 0.064 mg/ml
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzhydryl-amide 5-benzylamide
-
minimum inhibitory concentration above 0.032 mg/ml
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
minimum inhibitory concentration 0.003 mg/ml
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-benzylamide 3-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide]
-
minimum inhibitory concentration above 0.032 mg/ml
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide]
-
minimum inhibitory concentration 0.0005 mg/ml
1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] 3-[(tetrahydro-furan-2-yl)-amide]
-
minimum inhibitory concentration above 0.032 mg/ml
2,3-dihydrotriazolo[4,5-d]pyrimidine-5,7-dione
-
-
2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid
-
-
2-methyl-3-nitro-N-[3-(trifluoromethyl)phenyl]benzamide
-
50% inhibition at 0.00008 mM, wild type, 0.00037 mM, mutant R265A, 0.120, mutant H185A
2-methyl-N-1-naphthyl-3-nitrobenzamide
-
50% inhibition at 0.00008 mM, wild type, 0.00048 mM, mutant R265A, 0.180, mutant H185A
2-thioorotate
-
orotate analogue, 50% inhibition at 0.018 mM
3,4-dihydroxybenzoate
3,5-Dihydroxybenzoate
4,6-dioxo-1,4,5,6-tetrahydro-1,3,5-triazine-2-carboxylic acid
-
-
5-amino-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid
-
-
5-aminoorotate
-
orotate analogue, 50% inhibition at 1.6 mM
5-bromoorotate
-
orotate analogue, 50% inhibition at 0.016 mM
5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid
-
-
5-Fluoroorotate
-
orotate analogue, 50% inhibition at 0.055 mM
5-nitro-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid
-
-
5-nitroorotate
-
orotate analogue, 50% inhibition at 0.076 mM
5-[(dimethylamino)methyl]-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid
-
-
7,9-dihydro-3H-purine-2,6,8-trione
-
-
Barbiturate
-
dead-end inhibitor, competitive with respect to (S)-dihydroorotate
butyl 2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylate
-
-
leflunomide
-
cell line A20R resistant to leflunomide shows enhanced expression of enzyme to bypass the inhibitory effect, following long-time exposure, enzyme gene amplification can be assumed
Mercuric chloride
-
40% inhibition after 15 min at 0.000045 mM
methanol extract of brown algae Fucus evanescens
-
59% inhibition, noncompetitive
-
methanol extract of brown algae Pelvetia babingtonii
-
58% inhibition, noncompetitive
-
N-(2,4-dichlorophenyl)-2-naphthamide
-
50% inhibition at 0.00005 mM, wild type, 0.00008 mM, mutant R265A, above 0.05, mutant H185A
N-(2-fluorophenyl)naphthalene-2-carboxamide
-
50% inhibition at 0.00047 mM, wild type, 0.00030 mM, mutant R265A, 0.21, mutant H185A
N-(3,4-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00008 mM, wild type, 0.0028 mM, mutant R265A, 0.06, mutant H185A
N-(3,4-difluorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00026 mM, wild type, 0.00082 mM, mutant R265A, 0.25, mutant H185A
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00002 mM, wild type, 0.0004 mM, mutant R265A, 0.13, mutant H185A
N-(3-bromophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.00006 mM, wild type, 0.0012 mM, mutant R265A, 0.140, mutant H185A
N-(3-chloro-4-fluorophenyl)-2-methyl-3-nitrobenzamide
-
50% inhibition at 0.0001 mM, wild type, 0.0005 mM, mutant R265A, 0.13, mutant H185A
N-(4-bromo-2-methylphenyl)-2-naphthamide
-
50% inhibition at 0.00005 mM, wild type, 0.00005 mM, mutant R265A, 0.57, mutant H185A
N3-benzyl-1-(4-chlorophenyl)-N5-phenyl-1H-pyrazole-3,5-dicarboxamide
-
minimum inhibitory concentration 0.000125 mg/ml
Orotate
orotate methyl ester
-
orotate analogue, 50% inhibition at 0.71 mM
oxonate
crystallization data
oxonic acid
-
orotate analogue, 50% inhibition at 0.0099 mM
p-hydroxymercuribenzoate
-
98% inhibition after 5 min at 0.00227 mM
Salicylhydroxamic acid
-
weak inhibition, pH 9.0, 37°C
suramin
-
weak inhibition, pH 9.0, 37°C
Tiron
-
inhibits cytochrome c reduction and sulfite autoxidation
Uracil
-
orotate analogue, 50% inhibition at 2.5 mM
additional information
-