Application | Comment | Organism |
---|---|---|
drug development | MRSA PK is a potentially attractive drug target | Staphylococcus aureus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2-[(1E)-1-[2-(5-bromo-2-hydroxybenzoyl)hydrazinylidene]ethyl]-1-methyl-1H-indol-6-yl)dibromanium | - |
Staphylococcus aureus | |
2,4-dihydroxy-N'-[(E)-(2-hydroxy-6,7,8,9-tetrahydrodibenzo[b,d]furan-1-yl)methylidene]benzohydrazide | - |
Staphylococcus aureus | |
4-hydroxy-N'-(7-hydroxy-2,3-dihydro-8H-[1,4]dioxino[2,3-f]indol-8-yl)phthalazine-1-carbohydrazide | - |
Staphylococcus aureus | |
4-[(4-[3-[(1-hydroxy-2-methylpropan-2-yl)sulfamoyl]-4-methylphenyl]phthalazin-1-yl)amino]-N-methylbenzamide | - |
Staphylococcus aureus | |
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide | - |
Staphylococcus aureus | |
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]benzohydrazide | - |
Staphylococcus aureus | |
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)propylidene]benzohydrazide | - |
Staphylococcus aureus | |
5-bromo-2-hydroxy-N'-[(3E)-5-methyl-2-methylidene-1,2-dihydro-3H-indol-3-ylidene]benzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(1E)-1-(2,4-dihydroxyphenyl)ethylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(1E)-1-(5,6-difluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(1E)-1-(6-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(1E)-1-(6-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(1E)-1-(6-fluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
5-bromo-N'-[(3E)-5-bromo-2-methylidene-1,2-dihydro-3H-indol-3-ylidene]-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
additional information | development of highly potent inhibitors which demonstrate complete selectivity for the bacterial enzyme compared to all human orthologues, molecular docking, overview | Staphylococcus aureus | |
N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
N'-[(1E)-1-(2,4-dihydroxyphenyl)ethylidene]-3-(5,6-dimethyl-1,3-dihydro-2H-isoindol-2-yl)benzohydrazide | - |
Staphylococcus aureus | |
N'-[(3E)-5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxybenzohydrazide | - |
Staphylococcus aureus | |
N'-[(3Z)-1-ethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxynaphthalene-2-carbohydrazide | - |
Staphylococcus aureus | |
N-(4-methylphenyl)-2-[(4-sulfamoylphenyl)amino]pyridine-3-carboxamide | - |
Staphylococcus aureus |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Staphylococcus aureus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + pyruvate | Staphylococcus aureus | - |
ADP + phosphoenolpyruvate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Staphylococcus aureus | - |
a methicillin-resistant strain | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + pyruvate | - |
Staphylococcus aureus | ADP + phosphoenolpyruvate | - |
? |
Subunits | Comment | Organism |
---|---|---|
tetramer | structure-based molecular modeling and crystal structure analysis, overview | Staphylococcus aureus |
Synonyms | Comment | Organism |
---|---|---|
MRSA PK | - |
Staphylococcus aureus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Staphylococcus aureus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Staphylococcus aureus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000016 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-N'-[(1E)-1-(5,6-difluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | |
0.000045 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-N'-[(1E)-1-(6-fluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | |
0.000084 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]benzohydrazide | |
0.000091 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide | |
0.000114 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)propylidene]benzohydrazide | |
0.000165 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-N'-[(1E)-1-(6-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | |
0.000185 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | (2-[(1E)-1-[2-(5-bromo-2-hydroxybenzoyl)hydrazinylidene]ethyl]-1-methyl-1H-indol-6-yl)dibromanium | |
0.000228 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-N'-[(1E)-1-(6-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide | |
0.000381 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | 5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide | |
0.00091 | - |
pH not specified in the publication, 30°C | Staphylococcus aureus | N'-[(3Z)-1-ethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxynaphthalene-2-carbohydrazide |
General Information | Comment | Organism |
---|---|---|
metabolism | pyruvate kinase is a critical protein catalyzing the final step of glycolysis, which involves the transfer of a phosphoryl group from phosphoenolpyruvate to ADP, producing pyruvate and ATP | Staphylococcus aureus |