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Literature summary for 2.4.2.1 extracted from

  • Cattaneo, G.; Ubiali, D.; Calleri, E.; Rabuffetti, M.; Hoefner, G.C.; Wanner, K.T.; De Moraes, M.C.; Martinelli, L.K.B.; Santos, D.S.; Speranza, G.; Massolini, G.
    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 (2016), Anal. Chim. Acta, 943, 89-97 .
    View publication on PubMed

Inhibitors

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 [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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens P00491
-
-
Mycobacterium tuberculosis
-
-
-

Substrates and Products (Substrate)

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

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

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 [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Mycobacterium tuberculosis
37
-
assay at Homo sapiens

Turnover Number [1/s]

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

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 [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 [mM/s]

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