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Literature summary for 2.7.1.1 extracted from
- Thermal stabilty of glucokinase (GK) as influenced by the substrate glucose, an allosteric glucokinase activator drug (GKA) and the osmolytes glycerol and urea (2012), Biochim. Biophys. Acta, 1824, 769-784.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli as a GST-fusion protein | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| W167F/W257F | W99 kcat values are markedly lowered compared to wild-type, Km (ATP) increased compared to wild-type, kcat only moderately increased in the presence of glucokinase activator drug | Homo sapiens |
| W99R/W167F | W257 kcat values are markedly lowered compared to wild-type, Km (ATP) increased compared to wild-type | Homo sapiens |
| W99R/W257F | W167 kcat values onlye weakly lowered compared to wild-type, Km (ATP) weakly increased compared to wild-type, kcat increased in the presence of glucokinase activator drug | Homo sapiens |
General Stability
| General Stability | Organism |
|---|---|
| D-glucose stabilizes the enzyme through a specific, ligand induced intramolecular transition from an open to a closed conformation | Homo sapiens |
| glycerol increases the stability | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000023 | - |
ATP | wild-type in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens |  |
| 0.0000003 | - |
ATP | mutant W99R/W257F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000035 | - |
ATP | wild-type in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000046 | - |
ATP | wild-type, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000049 | - |
ATP | mutant W99R/W257F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000055 | - |
ATP | mutant W99R/W257F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000057 | - |
ATP | wild-type in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000071 | - |
ATP | mutant W167F/W257F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000071 | - |
ATP | mutant W99R/W167F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000078 | - |
ATP | mutant W99R/W257F, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000109 | - |
ATP | mutant W167F/W257F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000143 | - |
ATP | mutant W167F/W257F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000143 | - |
ATP | mutant W99R/W167F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000163 | - |
ATP | mutant W167F/W257F, pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000294 | - |
ATP | mutant W99R/W167F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 0.00000335 | - |
ATP | mutant W99R/W167F, pH and temperature not specified in the publication | Homo sapiens | |
Organic Solvent Stability
| Organic Solvent | Comment | Organism |
|---|---|---|
| Glycerol | glycerol causes large functional changes and increases stability as a result of generalized restructuring of surface water of glucokinase by an indirect mechanism and these changes can occur with minimal perturbation of the protein folding structure and with preservation of the unique cooperative kinetics of the enzyme whereas D-glucose stabilizes the enzyme through a specific, ligand induced intramolecular transition from an open to a closed conformation | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| pancreas | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + beta-D-glucose | - |
Homo sapiens | ADP + beta-D-glucose 6-phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| glucokinase 1 | - |
Homo sapiens |
Temperature Stability [°C]
| Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 40 | - |
stabilization by D-glucose and glycerol is limited since thermal glucokinase denaturation above 40 °C is irreversible even in their presence | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 5.9 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W167F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 6.1 | - |
beta-D-glucose | co-substrate: ATP, mutant W167F/W257F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 6.37 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W167F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 8.47 | - |
beta-D-glucose | co-substrate: ATP, mutant W167F/W257F, pH and temperature not specified in the publication | Homo sapiens | |
| 9.43 | - |
beta-D-glucose | co-substrate: ATP, mutant W167F/W257F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 11.1 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W167F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 12.4 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W167F, pH and temperature not specified in the publication | Homo sapiens | |
| 12.7 | - |
beta-D-glucose | co-substrate: ATP, mutant W167F/W257F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 26.2 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W257F in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 37.7 | - |
beta-D-glucose | co-substrate: ATP, wild-type in the presence of 20-30% glycerol, pH and temperature not specified in the publication | Homo sapiens | |
| 38.9 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W257F in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 60.5 | - |
beta-D-glucose | co-substrate: ATP, wild-type in the presence of 20-30% glycerol and in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 69.9 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W257F, pH and temperature not specified in the publication | Homo sapiens | |
| 83.7 | - |
beta-D-glucose | co-substrate: ATP, wild-type, pH and temperature not specified in the publication | Homo sapiens | |
| 91.3 | - |
beta-D-glucose | co-substrate: ATP, mutant W99R/W257F in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
| 166 | - |
beta-D-glucose | co-substrate: ATP, wild-type in the presence of 20 microM glucokinase activator drug (GKA), pH and temperature not specified in the publication | Homo sapiens | |
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