Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-(4-chloroanilino)-4-oxobutanoic acid | - |
Mus musculus | |
4-(4-chloroanilino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-(4-methylanilino)-4-oxobutanoic acid | - |
Mus musculus | |
4-(4-methylanilino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-(hexylamino)-4-oxobutanoic acid | - |
Mus musculus | |
4-(hexylamino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition, potent and selective inhibitor | Mus musculus | |
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition, potent and selective inhibitor | Rattus norvegicus | |
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition | Mus musculus | |
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition | Rattus norvegicus | |
4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Mus musculus | |
4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
glyceraldehyde 3-phosphate | about 80% inhibition at 2.5 mM, glyceraldehyde 3-phosphate is not a specific inhibitor of mGPDH but also alters succinate oxidation | Mus musculus | |
glyceraldehyde 3-phosphate | about 80% inhibition at 2.5 mM, glyceraldehyde 3-phosphate is not a specific inhibitor of mGPDH but also alters succinate oxidation | Rattus norvegicus | |
glycerone phosphate | product inhibition | Mus musculus | |
glycerone phosphate | product inhibition | Rattus norvegicus | |
methyl 4-(4-methylanilino)-4-oxobutanoate | - |
Mus musculus | |
methyl 4-(4-methylanilino)-4-oxobutanoate | - |
Rattus norvegicus | |
additional information | screening and identification of cell-permeant small-molecule inhibitors of mGPDH (iGP) discovered through small-molecule screening. Structure-activity analysis identifies a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulate both potency and off-target effects. The iGPs penetrate cellular membranes. Inhibitor selectivity, and effects of the inhibitors on kinetics of mGPDH, overview | Mus musculus | |
additional information | screening and identification of cell-permeant small-molecule inhibitors of mGPDH (iGP) discovered through small-molecule screening. Structure-activity analysis identifies a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulate both potency and off-target effects. The iGPs penetrate cellular membranes. Inhibitor selectivity, and effects of the inhibitors on kinetics of mGPDH, overview | Rattus norvegicus | |
N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide | - |
Mus musculus | |
N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide | - |
Rattus norvegicus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide | - |
Mus musculus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide | - |
Rattus norvegicus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide | - |
Mus musculus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide | - |
Rattus norvegicus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide | - |
Mus musculus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide | - |
Rattus norvegicus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide | - |
Mus musculus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide | - |
Rattus norvegicus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide | - |
Mus musculus | |
N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide | - |
Rattus norvegicus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the calcium-sensitive EF-hand domain of the enzyme lowers the Km for glycerol 3-phosphate as physiological levels of free calcium rise | Rattus norvegicus | |
additional information | - |
additional information | the calcium-sensitive EF-hand domain of the enzyme lowers the Km for glycerol 3-phosphate as physiological levels of free calcium rise | Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
mitochondrial inner membrane | the active site of mGPDH faces the mitochondrial intermembrane space, as does its calcium-sensitive EF-hand domain | Rattus norvegicus | 5743 | - |
mitochondrial inner membrane | the active site of mGPDH faces the mitochondrial intermembrane space, as does its calcium-sensitive EF-hand domain | Mus musculus | 5743 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
sn-glycerol 3-phosphate + ubiquinone | Rattus norvegicus | - |
glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | Mus musculus | - |
glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | Mus musculus C57BL/6 | - |
glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | Rattus norvegicus Wistar | - |
glycerone phosphate + ubiquinol | - |
ir |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | Q64521 | - |
- |
Mus musculus C57BL/6 | Q64521 | - |
- |
Rattus norvegicus | P35571 | - |
- |
Rattus norvegicus Wistar | P35571 | - |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
ubiquitination | mitochondrial sn-glycerol 3-phosphate dehydrogenase is a ubiquinone-linked enzyme | Rattus norvegicus |
ubiquitination | mitochondrial sn-glycerol 3-phosphate dehydrogenase is a ubiquinone-linked enzyme | Mus musculus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Mus musculus | - |
brain cortex | - |
Mus musculus | - |
hindlimb | - |
Rattus norvegicus | - |
skeletal muscle | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Rattus norvegicus | ? | - |
? | |
additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Mus musculus | ? | - |
? | |
additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Mus musculus C57BL/6 | ? | - |
? | |
additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Rattus norvegicus Wistar | ? | - |
? | |
sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Rattus norvegicus | ? | - |
? | |
sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Mus musculus | ? | - |
? | |
sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Mus musculus C57BL/6 | ? | - |
? | |
sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Rattus norvegicus Wistar | ? | - |
? | |
sn-glycerol 3-phosphate + ubiquinone | - |
Rattus norvegicus | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | - |
Mus musculus | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Rattus norvegicus | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Mus musculus | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | - |
Mus musculus C57BL/6 | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Mus musculus C57BL/6 | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | - |
Rattus norvegicus Wistar | glycerone phosphate + ubiquinol | - |
ir | |
sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Rattus norvegicus Wistar | glycerone phosphate + ubiquinol | - |
ir |
Synonyms | Comment | Organism |
---|---|---|
mGPDH | - |
Rattus norvegicus |
mGPDH | - |
Mus musculus |
mitochondrial sn-glycerol 3-phosphate dehydrogenase | - |
Rattus norvegicus |
mitochondrial sn-glycerol 3-phosphate dehydrogenase | - |
Mus musculus |
sn-glycerol 3-phosphate dehydrogenase | - |
Rattus norvegicus |
sn-glycerol 3-phosphate dehydrogenase | - |
Mus musculus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Rattus norvegicus |
37 | - |
assay at | Mus musculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ubiquinone | - |
Rattus norvegicus | |
ubiquinone | - |
Mus musculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics of iGP-1 and iGP-5 | Rattus norvegicus | |
additional information | - |
additional information | inhibition kinetics of iGP-1 and iGP-5 | Mus musculus | |
0.0007 | - |
4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | pH not specified in the publication, 37°C | Mus musculus | |
0.0095 | - |
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | pH not specified in the publication, 37°C | Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0007 | 0.001 | pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | |
0.003 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | |
0.005 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
0.0063 | 0.008 | pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
0.015 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | |
0.02 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | |
0.05 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
0.08 | - |
pH not specified in the publication, 37°C | Mus musculus | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide |
General Information | Comment | Organism |
---|---|---|
malfunction | despite the widespread expression of the enzyme, mGPDH-knockout mice display relatively mild phenotypes beyond weaning. These include decreased body mass and decreased white fat mass | Mus musculus |
physiological function | mitochondrial sn-glycerol 3-phosphate dehydrogenase (mGPDH) is a ubiquinone-linked enzyme in the mitochondrial inner membrane best characterized as part of the glycerol phosphate shuttle that transfers reducing equivalents from cytosolic NADH into the mitochondrial electron transport chain | Rattus norvegicus |
physiological function | mitochondrial sn-glycerol 3-phosphate dehydrogenase (mGPDH) is a ubiquinone-linked enzyme in the mitochondrial inner membrane best characterized as part of the glycerol phosphate shuttle that transfers reducing equivalents from cytosolic NADH into the mitochondrial electron transport chain | Mus musculus |