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Literature summary for 4.4.1.5 extracted from
- Glyoxalase I from Leishmania donovani: a potential target for anti-parasite drug (2005), Biochem. Biophys. Res. Commun., 337, 1237-1248.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | difference of the substrate specificity of the human and the Leishmania enzyme could be used for designing selective inhibitors against the parasite | Leishmania donovani |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Escherichia coli and Leishmania donovani | Leishmania donovani |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| flavone | IC50 wild type 56 microM, IC50 enzyme overexpressor 69 microM | Leishmania donovani |  |
| Lapachol | IC50 wild type 93 microM, IC50 enzyme overexpressor 96 microM | Leishmania donovani | |
| purpurogallin | IC50 wild type 70 microM, IC50 enzyme overexpressor 132 microM | Leishmania donovani | |
| quercetin | IC50 wild type 26 microM, IC50 enzyme overexpressor 27 microM | Leishmania donovani | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0284 | - |
reduced trypanothione | recombinant enzyme, pH 7.2, room temperature | Leishmania donovani | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ni2+ | - |
Leishmania donovani | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 23440 | - |
2 * 23440, SDS-PAGE | Leishmania donovani |
| 46000 | - |
SDS-PAGE, enzyme cross-linked with glutaraldehyde | Leishmania donovani |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Leishmania donovani | Q5XQR1 | recombinant enzyme | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Leishmania donovani |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.34 | - |
micromol/min/mg protein, native enzyme from crude lysate, pH 7.2, room temperature | Leishmania donovani |
| 3400 | - |
micromol/min/mg protein, recombinant enzyme, pH 7.2, room temperature | Leishmania donovani |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| trypanothione + methylglyoxal | - |
Leishmania donovani | S,S'-bis((R)-lactoyl)trypanothione | - |
r | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| dimer | 2 * 23440, SDS-PAGE | Leishmania donovani |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| GloI | - |
Leishmania donovani |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.026 | 0.027 | IC50 wild type 26 microM, IC50 enzyme overexpressor 27 microM | Leishmania donovani | quercetin | |
| 0.056 | - |
IC50 wild type 56 microM | Leishmania donovani | flavone | |
| 0.069 | - |
IC50 enzyme overexpressor 69 microM | Leishmania donovani | flavone | |
| 0.07 | - |
IC50 wild type 70 microM | Leishmania donovani | purpurogallin | |
| 0.093 | - |
IC50 wild type 93 microM | Leishmania donovani | Lapachol | |
| 0.096 | - |
IC50 enzyme overexpressor 96 microM | Leishmania donovani | Lapachol | |
| 0.132 | - |
IC50 enzyme overexpressor 132 microM | Leishmania donovani | purpurogallin | |
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