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Literature summary for 2.5.1.18 extracted from
- Design of potent inhibitors for Schistosoma japonica glutathione S-transferase (2006), Bioorg. Med. Chem., 14, 304-318.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of His-tagged enzyme in Escherichia coli | Schistosoma japonicum |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (17-chloro-3b-hydroxy-androsta-5,16-diene)-succinyl-glutathione | - |
Schistosoma japonicum |  |
| (S)-2-amino-4-cyanobutyric acid | - |
Schistosoma japonicum | |
| epiandrosterone-aspartyl-glutathione | - |
Schistosoma japonicum | |
| epiandrosterone-succinyl-glutathione | - |
Schistosoma japonicum | |
| gamma-glutamyl-(c-methoxycarbonyl)-alpha-glutamylglycine | - |
Schistosoma japonicum | |
| gamma-glutamyl-5-azanylidyne-L-norvalylglycine | - |
Schistosoma japonicum | |
| gamma-glutamyl-L-threonylglycine | - |
Schistosoma japonicum | |
| gamma-L-glutamyl-L-seryl-glycine | - |
Schistosoma japonicum | |
| additional information | implementation of both structure-based drug design and the concept of polyvalency to discover a series of potent and unsymmetrical GST inhibitors, stoichiometry of one inhibitor molecule per GST monomer via isothermal titration calorimetric measurement, overview, molecular modeling | Schistosoma japonicum | |
| N5-[(1S)-2-[(carboxymethyl)amino]-1-(cyanomethyl)-2-oxoethyl]glutamine | - |
Schistosoma japonicum | |
| prasterone-aspartyl-glutathione | - |
Schistosoma japonicum | |
| prasterone-succinyl-glutathione | - |
Schistosoma japonicum | |
| [(3aR,5R,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-succinyl-glutathione | - |
Schistosoma japonicum | |
| [(3aR,5S,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-aspartyl-glutathione | - |
Schistosoma japonicum | |
| [(3aR,5S,7aR)-3a,5-dihydroxy-7a-methyloctahydro-1H-inden-1-one]-succinyl-glutathione | - |
Schistosoma japonicum | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Schistosoma japonicum | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged enzyme from Escherichia coli by nickel affinity chromatography | Schistosoma japonicum |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| glutathione S-transferase | - |
Schistosoma japonicum |
| GST | - |
Schistosoma japonicum |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Schistosoma japonicum |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 6.5 | - |
assay at | Schistosoma japonicum |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.147 | - |
pH 6.5, 30°C | Schistosoma japonicum | N5-[(1S)-2-[(carboxymethyl)amino]-1-(cyanomethyl)-2-oxoethyl]glutamine | |
| 0.395 | - |
pH 6.5, 30°C | Schistosoma japonicum | (S)-2-amino-4-cyanobutyric acid | |
| 0.774 | - |
pH 6.5, 30°C | Schistosoma japonicum | gamma-glutamyl-(c-methoxycarbonyl)-alpha-glutamylglycine | |
| 1.5 | - |
above, pH 6.5, 30°C | Schistosoma japonicum | gamma-glutamyl-L-threonylglycine | |
| 3 | - |
above, pH 6.5, 30°C | Schistosoma japonicum | gamma-glutamyl-5-azanylidyne-L-norvalylglycine | |
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Release 2023.1 (January 2023)
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