Inhibitors | Comment | Organism | Structure |
---|---|---|---|
8-Bromoadenosine | about 30% inhibition | Homo sapiens | |
8-Bromoguanosine | about 30% inhibition | Homo sapiens | |
8-Bromoguanosine | about 25% inhibition | Mycobacterium tuberculosis | |
8-dimethylaminoinosine | about 20% inhibition | Homo sapiens | |
8-methoxyinosine | about 20% inhibition | Mycobacterium tuberculosis | |
8-methylaminoinosine | about 30% inhibition | Homo sapiens | |
8-methylaminoinosine | about 25% inhibition | Mycobacterium tuberculosis | |
acyclovir | about 40% inhibition | Homo sapiens | |
acyclovir | about 35% inhibition | Mycobacterium tuberculosis | |
additional information | development, validation, and application of a 96-well enzymatic assay based on LC-ESI-MS/MS quantification for the screening of selective inhibitors against Mycobacterium tuberculosis purine nucleoside phosphorylase, overview. Evaluation of a set of 8-halo-, 8-amino-, 8-O-alkyl-substituted purine ribonucleosides synthesized on purpose as potential inhibitors against MtbPNP. The assayed 8-substituted ribonucleosides do not exert a significant inhibitory effect against the tested enzymes up to 1 mM. No or poor inhibition by formycin A (an inhibitor of hexameric PNP), 8-ethylaminoinosine, 8-methoxyinosine, and 8-ethoxyinosine | Homo sapiens | |
additional information | development, validation, and application of a 96-well enzymatic assay based on LC-ESI-MS/MS quantification for the screening of selective inhibitors against Mycobacterium tuberculosis purine nucleoside phosphorylase, overview. Evaluation of a set of 8-halo-, 8-amino-, 8-O-alkyl-substituted purine ribonucleosides synthesized on purpose as potential inhibitors against MtbPNP. The assayed 8-substituted ribonucleosides do not exert a significant inhibitory effect against the tested enzymes up to 1 mM. No or poor inhibition by formycin A (an inhibitor of hexameric PNP), 8-bromoadenosine, 8-ethylaminoinosine, 8-dimethylaminoinosine, and 8-ethoxyinosine | Mycobacterium tuberculosis |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Mycobacterium tuberculosis | |
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
0.06 | - |
Inosine | pH 7.5, 37°C | Mycobacterium tuberculosis | |
0.15 | - |
phosphate | pH 7.5, 37°C | Mycobacterium tuberculosis | |
0.15 | - |
Inosine | pH 7.5, 37°C | Homo sapiens | |
0.66 | - |
phosphate | pH 7.5, 37°C | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
inosine + phosphate | Mycobacterium tuberculosis | complete conversion | hypoxanthine + alpha-D-ribose 1-phosphate | - |
r | |
inosine + phosphate | Homo sapiens | complete conversion | hypoxanthine + alpha-D-ribose 1-phosphate | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P00491 | - |
- |
Mycobacterium tuberculosis | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
inosine + phosphate | complete conversion | Mycobacterium tuberculosis | hypoxanthine + alpha-D-ribose 1-phosphate | - |
r | |
inosine + phosphate | complete conversion | Homo sapiens | hypoxanthine + alpha-D-ribose 1-phosphate | - |
r |
Subunits | Comment | Organism |
---|---|---|
homotrimer | - |
Mycobacterium tuberculosis |
homotrimer | - |
Homo sapiens |
More | the enzyme appears to have transition states | Mycobacterium tuberculosis |
More | the enzyme appears to have transition states | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
MtbPNP | - |
Mycobacterium tuberculosis |
MtbPNP | - |
Homo sapiens |
PNP | - |
Mycobacterium tuberculosis |
PNP | - |
Homo sapiens |
purine nucleoside phosphorylase | - |
Mycobacterium tuberculosis |
purine nucleoside phosphorylase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Mycobacterium tuberculosis |
37 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
4.5 | - |
phosphate | pH 7.5, 37°C | Mycobacterium tuberculosis | |
14 | - |
Inosine | pH 7.5, 37°C | Homo sapiens | |
15.7 | - |
Inosine | pH 7.5, 37°C | Mycobacterium tuberculosis | |
76 | - |
phosphate | pH 7.5, 37°C | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Mycobacterium tuberculosis |
7.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Mycobacterium tuberculosis | |
additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
0.028 | - |
acyclovir | pH 7.5, 37°C | Mycobacterium tuberculosis |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
30 | - |
phosphate | pH 7.5, 37°C | Mycobacterium tuberculosis | |
93.3 | - |
Inosine | pH 7.5, 37°C | Homo sapiens | |
115.15 | - |
phosphate | pH 7.5, 37°C | Homo sapiens | |
261.7 | - |
Inosine | pH 7.5, 37°C | Mycobacterium tuberculosis |