Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.3.5.2 extracted from

  • Nonato, M.C.; de Padua, R.A.P.; David, J.S.; Reis, R.A.G.; Tomaleri, G.P.; DMuniz Pereira, H.; Calil, F.A.
    Structural basis for the design of selective inhibitors for Schistosoma mansoni dihydroorotate dehydrogenase (2019), Biochimie, 158, 180-190 .
    View publication on PubMed
Search for more literature for 1.3.5.2

Crystallization (Commentary)

Crystallization (Comment) Organism
comparison of ligand-free forms of Schistosoma mansoni DHODH and human DHODH, which undergo different rearrangements in solution Homo sapiens
homology modeling, presence of an additional protuberant domain predicted to fold as a flexible loop and absent in the other known class 2 DHODHs. The ligand-free forms of Schistosoma mansoni DHODH and human DHODH undergo different rearrangements in solution Schistosoma mansoni

Inhibitors

Inhibitors Comment Organism Structure
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine i.e. DSM265 Homo sapiens
2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine i.e. DSM265 Schistosoma mansoni
atovaquone
-
 Homo sapiens
atovaquone
-
 Schistosoma mansoni
brequinar
-
 Homo sapiens
brequinar
-
 Schistosoma mansoni
teriflunomide
-
 Homo sapiens
teriflunomide
-
 Schistosoma mansoni

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.17
-
 coenzyme Q0 pH 8.2, 25°C Schistosoma mansoni
0.23
-
 dihydroorotate pH 8.2, 25°C Schistosoma mansoni
0.29
-
 dihydroorotate pH 8.2, 25°C Homo sapiens
0.35
-
 coenzyme Q0 pH 8.2, 25°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
 Homo sapiens 5739
-
mitochondrion
-
 Schistosoma mansoni 5739
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q02127
-
-
Schistosoma mansoni G4VFD7
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dihydroorotate + coenzyme Q0
-
 Homo sapiens orotate + reduced coenzyme Q0
-
 ?
dihydroorotate + coenzyme Q0
-
 Schistosoma mansoni orotate + reduced coenzyme Q0
-
 ?

Synonyms

Synonyms Comment Organism
DHODH
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.78
-
 dihydroorotate pH 8.2, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000037
-
 pH 8.2, 25°C Homo sapiens brequinar
0.00032
-
 pH 8.2, 25°C Homo sapiens teriflunomide
0.00043
-
 pH 8.2, 25°C Schistosoma mansoni atovaquone
0.0026
-
 pH 8.2, 25°C Homo sapiens atovaquone
0.007
-
 pH 8.2, 25°C Homo sapiens 2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.02
-
 pH 8.2, 25°C Schistosoma mansoni brequinar
0.021
-
 pH 8.2, 25°C Schistosoma mansoni 2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-lambda6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
0.05
-
 pH 8.2, 25°C Schistosoma mansoni teriflunomide

General Information

General Information Comment Organism
physiological function enzyme employs a two-site Ping-Pong steady-state mechanism of catalysis. In the first and reductive half-reaction, the enzyme oxidizes dihydroorotate to orotate with the concomitant reduction of FMN to FMNH2. In the second and oxidative half-reaction, FMNH2 is reoxidized by reducing the quinone to quinol Schistosoma mansoni