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Literature summary for 3.4.21.26 extracted from
- Engineering a thermostable human prolyl endopeptidase for antibody-directed enzyme prodrug therapy (2004), Biochemistry, 43, 6293-6303.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | use of enzyme in antibody-directed enzyme prodrug therapy strategy, ADEPT. Coupling of enzyme mutant E289G to human antibody specific to the EDB domain of fibronectin, conjugate retains antigen binding and enzymatic activity | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| E289G | improved protein stability, 4fold longer half-life at 37°C compared to wild-type | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
recombinant enzyme | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| native enzyme expressed in Escherichia coli is rapidly thermally inactivated. Mutation E289G improves protein stability | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.096 | - |
pH 7.4, 22°C, substrate benzyloxycarbonyl-Gly-L-Pro-doxorubicin | Homo sapiens |
| 0.813 | - |
pH 7.4, 22°C, substrate benzyloxycarbonyl-Gly-L-Pro-melphalan | Homo sapiens |
| 4.066 | - |
pH 7.4, 22°C, substrate benzyloxycarbonyl-Gly-L-Pro-7-amido-4-methylcoumarin | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| benzyloxycarbonyl-Gly-L-Pro-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | benzyloxycarbonyl-Gly-L-Pro + 7-amino-4-methylcoumarin | - |
? |  |
| benzyloxycarbonyl-Gly-L-Pro-doxorubicin + H2O | - |
Homo sapiens | benzyloxycarbonyl-Gly-L-Pro + doxorubicin | - |
? | |
| benzyloxycarbonyl-Gly-L-Pro-melphalan + H2O | - |
Homo sapiens | benzyloxycarbonyl-Gly-L-Pro + melphalan | - |
? | |
Temperature Stability [°C]
| Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 34 | - |
wild-type, 50% loss of activy in 30 min | Homo sapiens |
| 37 | - |
wild-type, 20 min, 15% loss of activity in phosphate-buffered saline, 69% loss of activiy in human serum | Homo sapiens |
| 43 | - |
mutant E289G, 50% loss of activity in 30 min | Homo sapiens |
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