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Literature summary for 2.4.2.1 extracted from
- Characterization of an engineered human purine nucleoside phosphorylase fused to an anti-her2/neu single chain Fv for use in ADEPT (2009), J. Exp. Clin. Cancer Res., 28, 147.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | use of mutant E201Q/N243D in Antibody Dependent Enzyme Prodrug Therapy ADEPT by fusion to the human anti-HER2/neu single chain Fv. In vitro the construct binds specifically to HER2/neu expressing tumor cells and localizes the enzyme to tumor cells, where the enzymatic activity of the mutant, but not the wild type enzyme, results in phosphorolysis of the prodrug, 2-fluoro-2'-deoxyadenosine to the cytotoxic drug 2-fluoroadenine causing inhibition of tumor cell proliferation | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| E201Q/N243D | unlike wild-type, mutant is able to cleave prodrugs 2-fluoro-2'-deoxyadenosine, Cladribine, and 2-fluoroadenosine | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.059 | - |
guanosine | mutant E201Q/N243D | Homo sapiens |  |
| 0.264 | - |
2-fluoro-2'-deoxyadenosine | mutant E201Q/N243D | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2-fluoro-2-deoxyadenosine + phosphate | no substrate for wild-type, substrate of double mutant E201Q/N243D | Homo sapiens | adenine + 2-fluoro-2-deoxy-alpha-D-ribose 1-phosphate | - |
? | |
| guanosine + phosphate | - |
Homo sapiens | guanine + alpha-D-ribose 1-phosphate | - |
? | |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.155 | - |
2-fluoro-2'-deoxyadenosine | mutant E201Q/N243D | Homo sapiens | |
| 60 | - |
guanosine | mutant E201Q/N243D | Homo sapiens | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 568 | - |
2-fluoro-2'-deoxyadenosine | mutant E201Q/N243D | Homo sapiens | |
| 1020 | - |
guanosine | mutant E201Q/N243D | Homo sapiens | |
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