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Literature summary for 2.4.2.1 extracted from
- Hydroxyl-related differences for three dietary flavonoids as inhibitors of human purine nucleoside phosphorylase (2018), Int. J. Biol. Macromol., 118, 588-598 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| apigenin | 77.4% inhibition at 0.15 mM, reversible inhibition | Homo sapiens |  |
| baicalein | 72% inhibition at 0.15 mM, reversible inhibition | Homo sapiens | |
| chrysin | 5,7-dihydroxyflavone, a natural flavone found in various plant extracts, including blue passionflower, honey and propolis, etc., 38.8% inhibition at 0.15 mM, reversible inhibition | Homo sapiens | |
| forodesine hydrochloride | - |
Homo sapiens | |
| additional information | the hydroxylation on position C4' of chrysin (-> apigenin) mildly decreases the binding affinities for PNP, whereas on the position C6 of chrysin (-> baicalein) it significantly increases binding affinities. The hydroxylation on position C4' and C6 greatly improves their PNP inhibitory effects. Results from molecular modeling reveal that there are two binding sites, i.e. active site (major) and tryptophan site (minor) on PNP, and the binding of these flavonoids might induce a serious conformational destabilization of PNP as a result of altering the microenvironment and morphology by flavonoids. Docking analysis of chrysin, baicalein or apigenin with PNP at 25°C, overview | Homo sapiens | |
| ulodesine | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| guanosine + phosphate | Homo sapiens | - |
guanine + alpha-D-ribose 1-phosphate | - |
r | |
| inosine + phosphate | Homo sapiens | - |
hypoxanthine + alpha-D-ribose 1-phosphate | - |
r | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P00491 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| guanosine + phosphate | - |
Homo sapiens | guanine + alpha-D-ribose 1-phosphate | - |
r | |
| inosine + phosphate | - |
Homo sapiens | hypoxanthine + alpha-D-ribose 1-phosphate | - |
r | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| homohexamer | - |
Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PNP | - |
Homo sapiens |
| purine nucleoside phosphorylase | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | 37 | assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0609 | - |
pH 7.4, 37°C | Homo sapiens | apigenin | |
| 0.0894 | - |
pH 7.4, 37°C | Homo sapiens | baicalein | |
| 0.213 | - |
pH 7.4, 37°C | Homo sapiens | chrysin | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| metabolism | purine nucleoside phosphorylase (PNP) is a crucial enzyme that participates in the metabolism of purines in nucleoside salvage pathway | Homo sapiens |
| additional information | results from molecular modeling reveal that there are two binding sites, i.e. active site (major) and tryptophan site (minor) on PNP. Analysis of structure-activity relationship, computational modeling, binding structure in the active site, overview | Homo sapiens |
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