EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.1.1.8 | additional information | no inhibition of the cytosolic NAD+-linked cGPDH enzyme by cell-permeant small-molecule inhibitors of mitochondrial mGPDH, EC 1.1.5.3, with a core benzimidazole-phenyl-succinamide structure | Oryctolagus cuniculus | |
1.1.5.3 | 4-(4-chloroanilino)-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-(4-chloroanilino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-(4-methylanilino)-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-(4-methylanilino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-(hexylamino)-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-(hexylamino)-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition, potent and selective inhibitor | Mus musculus | |
1.1.5.3 | 4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition, potent and selective inhibitor | Rattus norvegicus | |
1.1.5.3 | 4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition | Mus musculus | |
1.1.5.3 | 4-[4-(1H-naphtho[2,3-d]imidazol-2-yl)anilino]-4-oxobutanoic acid | mixed type inhibition | Rattus norvegicus | |
1.1.5.3 | 4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[4-[5-(3-carboxypropanamido)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Mus musculus | |
1.1.5.3 | 4-[4-[5-(cyclohexa-2,4-diene-1-carbonyl)-1H-benzimidazol-2-yl]anilino]-4-oxobutanoic acid | - |
Rattus norvegicus | |
1.1.5.3 | 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 | |
1.1.5.3 | 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 | |
1.1.5.3 | glycerone phosphate | product inhibition | Mus musculus | |
1.1.5.3 | glycerone phosphate | product inhibition | Rattus norvegicus | |
1.1.5.3 | methyl 4-(4-methylanilino)-4-oxobutanoate | - |
Mus musculus | |
1.1.5.3 | methyl 4-(4-methylanilino)-4-oxobutanoate | - |
Rattus norvegicus | |
1.1.5.3 | 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 | |
1.1.5.3 | 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 | |
1.1.5.3 | N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(1H-naphtho[2,3-d]imidazol-2-yl)phenyl]butanamide | - |
Rattus norvegicus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-2-oxopropanamide | - |
Rattus norvegicus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-3-methylbutanamide | - |
Rattus norvegicus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]-4-ethoxybenzamide | - |
Rattus norvegicus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]cyclopropanecarboxamide | - |
Rattus norvegicus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide | - |
Mus musculus | |
1.1.5.3 | N-[4-(5,6-dihydro-1H-benzimidazol-2-yl)phenyl]furan-2-carboxamide | - |
Rattus norvegicus |
EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
1.1.5.3 | 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 | |
1.1.5.3 | 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 |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
1.1.1.8 | cytosol | - |
Oryctolagus cuniculus | 5829 | - |
1.1.1.8 | soluble | - |
Oryctolagus cuniculus | - |
- |
1.1.5.3 | mitochondrial inner membrane | the active site of mGPDH faces the mitochondrial intermembrane space, as does its calcium-sensitive EF-hand domain | Rattus norvegicus | 5743 | - |
1.1.5.3 | mitochondrial inner membrane | the active site of mGPDH faces the mitochondrial intermembrane space, as does its calcium-sensitive EF-hand domain | Mus musculus | 5743 | - |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.1.1.8 | sn-glycerol 3-phosphate + NAD+ | Oryctolagus cuniculus | - |
glycerone phosphate + NADH + H+ | - |
r | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | Rattus norvegicus | - |
glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | Mus musculus | - |
glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | Mus musculus C57BL/6 | - |
glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | Rattus norvegicus Wistar | - |
glycerone phosphate + ubiquinol | - |
ir |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.1.1.8 | Oryctolagus cuniculus | P08507 | - |
- |
1.1.5.3 | Mus musculus | Q64521 | - |
- |
1.1.5.3 | Mus musculus C57BL/6 | Q64521 | - |
- |
1.1.5.3 | Rattus norvegicus | P35571 | - |
- |
1.1.5.3 | Rattus norvegicus Wistar | P35571 | - |
- |
EC Number | Posttranslational Modification | Comment | Organism |
---|---|---|---|
1.1.5.3 | ubiquitination | mitochondrial sn-glycerol 3-phosphate dehydrogenase is a ubiquinone-linked enzyme | Rattus norvegicus |
1.1.5.3 | ubiquitination | mitochondrial sn-glycerol 3-phosphate dehydrogenase is a ubiquinone-linked enzyme | Mus musculus |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
1.1.1.8 | commercial preparation | purified enzyme | Oryctolagus cuniculus | - |
1.1.1.8 | skeletal muscle | - |
Oryctolagus cuniculus | - |
1.1.5.3 | brain | - |
Mus musculus | - |
1.1.5.3 | brain cortex | - |
Mus musculus | - |
1.1.5.3 | hindlimb | - |
Rattus norvegicus | - |
1.1.5.3 | skeletal muscle | - |
Rattus norvegicus | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.1.1.8 | sn-glycerol 3-phosphate + NAD+ | - |
Oryctolagus cuniculus | glycerone phosphate + NADH + H+ | - |
r | |
1.1.1.8 | sn-glycerol 3-phosphate + NAD+ | NAD+-linked cGPDH can interconvert DHAP and glycerol 3-phosphate | Oryctolagus cuniculus | glycerone phosphate + NADH + H+ | - |
r | |
1.1.5.3 | additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Rattus norvegicus | ? | - |
? | |
1.1.5.3 | additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Mus musculus | ? | - |
? | |
1.1.5.3 | additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Mus musculus C57BL/6 | ? | - |
? | |
1.1.5.3 | additional information | usage of an assay method specific for superoxide/H2O2 production by mGPDH | Rattus norvegicus Wistar | ? | - |
? | |
1.1.5.3 | sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Rattus norvegicus | ? | - |
? | |
1.1.5.3 | sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Mus musculus | ? | - |
? | |
1.1.5.3 | sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Mus musculus C57BL/6 | ? | - |
? | |
1.1.5.3 | sn-glycerol 3-phosphate + 2,6-dichlorophenolindophenol | - |
Rattus norvegicus Wistar | ? | - |
? | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | - |
Rattus norvegicus | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | - |
Mus musculus | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Rattus norvegicus | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Mus musculus | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | - |
Mus musculus C57BL/6 | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Mus musculus C57BL/6 | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | - |
Rattus norvegicus Wistar | glycerone phosphate + ubiquinol | - |
ir | |
1.1.5.3 | sn-glycerol 3-phosphate + ubiquinone | the ubiquinone-linked reaction catalyzed by mGPDH is irreversible | Rattus norvegicus Wistar | glycerone phosphate + ubiquinol | - |
ir |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.1.1.8 | cGPdH | - |
Oryctolagus cuniculus |
1.1.1.8 | cytosolic GPDH | - |
Oryctolagus cuniculus |
1.1.1.8 | GPD1 | - |
Oryctolagus cuniculus |
1.1.5.3 | mGPDH | - |
Rattus norvegicus |
1.1.5.3 | mGPDH | - |
Mus musculus |
1.1.5.3 | mitochondrial sn-glycerol 3-phosphate dehydrogenase | - |
Rattus norvegicus |
1.1.5.3 | mitochondrial sn-glycerol 3-phosphate dehydrogenase | - |
Mus musculus |
1.1.5.3 | sn-glycerol 3-phosphate dehydrogenase | - |
Rattus norvegicus |
1.1.5.3 | sn-glycerol 3-phosphate dehydrogenase | - |
Mus musculus |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
1.1.1.8 | 37 | - |
assay at | Oryctolagus cuniculus |
1.1.5.3 | 37 | - |
assay at | Rattus norvegicus |
1.1.5.3 | 37 | - |
assay at | Mus musculus |
EC Number | Cofactor | Comment | Organism | Structure |
---|---|---|---|---|
1.1.1.8 | NAD+ | - |
Oryctolagus cuniculus | |
1.1.1.8 | NADH | - |
Oryctolagus cuniculus | |
1.1.5.3 | ubiquinone | - |
Rattus norvegicus | |
1.1.5.3 | ubiquinone | - |
Mus musculus |
EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|---|
1.1.5.3 | additional information | - |
additional information | inhibition kinetics of iGP-1 and iGP-5 | Rattus norvegicus | |
1.1.5.3 | additional information | - |
additional information | inhibition kinetics of iGP-1 and iGP-5 | Mus musculus | |
1.1.5.3 | 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 | |
1.1.5.3 | 0.0095 | - |
4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | pH not specified in the publication, 37°C | Mus musculus |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
1.1.5.3 | 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 | |
1.1.5.3 | 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 | |
1.1.5.3 | 0.005 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(5-methyl-1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
1.1.5.3 | 0.0063 | 0.008 | pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
1.1.5.3 | 0.015 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1,3-benzothiazol-2-yl)anilino]-4-oxobutanoic acid | |
1.1.5.3 | 0.02 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[4-(1,3-benzoxazol-2-yl)anilino]-4-oxobutanoic acid | |
1.1.5.3 | 0.05 | - |
pH not specified in the publication, 37°C | Mus musculus | 4-[3-(1H-benzimidazol-2-yl)anilino]-4-oxobutanoic acid | |
1.1.5.3 | 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 |
EC Number | General Information | Comment | Organism |
---|---|---|---|
1.1.5.3 | 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 |
1.1.5.3 | 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 |
1.1.5.3 | 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 |