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Literature summary extracted from

  • Baldwin, J.; Michnoff, C.H.; Malmquist, N.A.; White, J.; Roth, M.G.; Rathod, P.K.; Phillips, M.A.
    High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase (2005), J. Biol. Chem., 280, 21847-21853.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.3.5.2 H185A 4fold increase in KM-value of CoQD, 50% increase in KM-value of L-dihydroorotate Plasmodium falciparum
1.3.5.2 R265A 2fold increase in KM-value of CoQD, 15% increase in KM-value of L-dihydroorotate Plasmodium falciparum
1.3.98.1 H185A 4fold increase in KM-value of CoQD, 50% increase in KM-value of L-dihydroorotate Plasmodium falciparum
1.3.98.1 R265A 2fold increase in KM-value of CoQD, 15% increase in KM-value of L-dihydroorotate Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 1-(2-methoxyphenyl)-3-(1-naphthyl)urea 50% inhibition at 0.00023 mM, wild type, 0.00024 mM, mutant R265A, 0.140, mutant H185A Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 2-methyl-N-1-naphthyl-3-nitrobenzamide 50% inhibition at 0.00008 mM, wild type, 0.00048 mM, mutant R265A, 0.180, mutant H185A Plasmodium falciparum
1.3.5.2 N-(2,4-dichlorophenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00008 mM, mutant R265A, above 0.05, mutant H185A Plasmodium falciparum
1.3.5.2 N-(2-fluorophenyl)-2-naphthamide 50% inhibition at 0.00047 mM, wild type, 0.00030 mM, mutant R265A, 0.21, mutant H185A Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 N-(3-bromophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00006 mM, wild type, 0.0012 mM, mutant R265A, 0.140, mutant H185A Plasmodium falciparum
1.3.5.2 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 Plasmodium falciparum
1.3.5.2 N-(4-bromo-2-methylphenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00005 mM, mutant R265A, 0.57, mutant H185A Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 1-(2-methoxyphenyl)-3-(1-naphthyl)urea 50% inhibition at 0.00023 mM, wild type, 0.00024 mM, mutant R265A, 0.140, mutant H185A Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 2-methyl-N-1-naphthyl-3-nitrobenzamide 50% inhibition at 0.00008 mM, wild type, 0.00048 mM, mutant R265A, 0.180, mutant H185A Plasmodium falciparum
1.3.98.1 N-(2,4-dichlorophenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00008 mM, mutant R265A, above 0.05, mutant H185A Plasmodium falciparum
1.3.98.1 N-(2-fluorophenyl)naphthalene-2-carboxamide 50% inhibition at 0.00047 mM, wild type, 0.00030 mM, mutant R265A, 0.21, mutant H185A Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 N-(3-bromophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00006 mM, wild type, 0.0012 mM, mutant R265A, 0.140, mutant H185A Plasmodium falciparum
1.3.98.1 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 Plasmodium falciparum
1.3.98.1 N-(4-bromo-2-methylphenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00005 mM, mutant R265A, 0.57, mutant H185A Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.3.5.2 0.016
-
 decylubiquinone pH 8.0, 22°C, wild-type Plasmodium falciparum
1.3.5.2 0.032
-
 decylubiquinone pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.5.2 0.066
-
 decylubiquinone pH 8.0, 22°C, mutant H185A Plasmodium falciparum
1.3.5.2 0.091
-
 L-dihydroorotate pH 8.0, 22°C, wild-type Plasmodium falciparum
1.3.5.2 0.105
-
 L-dihydroorotate pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.5.2 0.123
-
 L-dihydroorotate pH 8.0, 22°C, mutant H185A Plasmodium falciparum
1.3.98.1 0.016
-
 CoQ pH 8.0, 22°C, wild-type Plasmodium falciparum
1.3.98.1 0.032
-
 CoQ pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.98.1 0.066
-
 CoQ pH 8.0, 22°C, mutant H185A Plasmodium falciparum
1.3.98.1 0.091
-
 L-dihydroorotate pH 8.0, 22°C, wild-type Plasmodium falciparum
1.3.98.1 0.105
-
 L-dihydroorotate pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.98.1 0.123
-
 L-dihydroorotate pH 8.0, 22°C, mutant H185A Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
1.3.5.2 Plasmodium falciparum
-
-
-
1.3.98.1 Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.5.2 L-dihydroorotate + 2,6-dichloroindophenol
-
 Plasmodium falciparum orotate + ?
-
 ?
1.3.5.2 L-dihydroorotate + decylubiquinone
-
 Plasmodium falciparum orotate + ?
-
 ?
1.3.98.1 L-dihydroorotate + 2,6-dichloroindophenol
-
 Plasmodium falciparum orotate + ?
-
 ?
1.3.98.1 L-dihydroorotate + CoQ
-
 Plasmodium falciparum orotate + ?
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.3.5.2 1.7
-
 L-dihydroorotate pH 8.0, 22°C, mutant H185A Plasmodium falciparum
1.3.5.2 4.6
-
 L-dihydroorotate pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.5.2 7.8
-
 L-dihydroorotate pH 8.0, 22°C, wild-type Plasmodium falciparum
1.3.98.1 1.7
-
 L-dihydroorotate pH 8.0, 22°C, mutant H185A Plasmodium falciparum
1.3.98.1 4.6
-
 L-dihydroorotate pH 8.0, 22°C, mutant R265A Plasmodium falciparum
1.3.98.1 7.8
-
 L-dihydroorotate pH 8.0, 22°C, wild-type Plasmodium falciparum