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Literature summary extracted from
- Development of a selective and highly sensitive fluorescence assay for nucleoside triphosphate diphosphohydrolase1 (NTPDase1, CD39) (2018), Analyst, 143, 5417-5430 .
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.6.1.5 | medicine | activation of CD39 has potential for treating inflammatory diseases, while inhibition is suggested as a strategy for the immunotherapy of cancer | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.6.1.5 | ARL67156 | - |
Homo sapiens |  |
| 3.6.1.5 | levamisole | - |
Homo sapiens | |
| 3.6.1.5 | PSB-POM141 | i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8- | Homo sapiens | |
| 3.6.1.5 | Reactive blue 2 | - |
Homo sapiens | |
| 3.6.1.5 | theophylline | - |
Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.6.1.5 | 0.0133 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase3 | Homo sapiens | |
| 3.6.1.5 | 0.0196 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase1 | Homo sapiens | |
| 3.6.1.5 | 0.0555 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase2 | Homo sapiens | |
| 3.6.1.5 | 0.105 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase8 | Homo sapiens | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.6.1.5 | Homo sapiens | O75355 | - |
- |
| 3.6.1.5 | Homo sapiens | P49961 | - |
- |
| 3.6.1.5 | Homo sapiens | Q5MY95 | - |
- |
| 3.6.1.5 | Homo sapiens | Q9Y5L3 | - |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.6.1.5 | N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate + H2O | developement of a selective and highly sensitive capillary electrophoresis (CE) assay using a fluorescent CD39 substrate, a fluorescein-labelled ATP, i.e. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate that is converted to its AMP derivative (N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate). To accelerate the assays, a two-directional (forward and reverse) CE system is implemented using 96-well plates, which is suitable for the screening of compound libraries. Achievement of a large enhancement in sensitivity as compared to previous methods (e.g. malachite-green assay: 1000000fold, CE-UV assay: 500000fold, fluorescence polarization immunoassay: 12500fold). The assay is validated by performing inhibition assays with several standard CD39 inhibitors. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate is preferably hydrolyzed by CD39 as compared to other ectonucleotidases | Homo sapiens | N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate + diphosphate | - |
ir | |
| 3.6.1.5 | N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate + H2O | i.e. PSB-170621A, developement of a selective and highly sensitive capillary electrophoresis (CE) assay using a fluorescent CD39 substrate, a fluorescein-labelled ATP, i.e. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate that is converted to its AMP derivative (N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate). To accelerate the assays, a two-directional (forward and reverse) CE system is implemented using 96-well plates, which is suitable for the screening of compound libraries. Achievement of a large enhancement in sensitivity as compared to previous methods (e.g. malachite-green assay: 1000000fold, CE-UV assay: 500000fold, fluorescence polarization immunoassay: 12500fold). The assay is validated by performing inhibition assays with several standard CD39 inhibitors. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate is preferably hydrolyzed by CD39 as compared to other ectonucleotidases | Homo sapiens | N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate + diphosphate | - |
ir | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.6.1.5 | CD39 | - |
Homo sapiens |
| 3.6.1.5 | ecto-nucleoside triphosphate diphosphohydrolase1 | - |
Homo sapiens |
| 3.6.1.5 | ecto-nucleoside triphosphate diphosphohydrolase2 | - |
Homo sapiens |
| 3.6.1.5 | ecto-nucleoside triphosphate diphosphohydrolase3 | - |
Homo sapiens |
| 3.6.1.5 | ecto-nucleoside triphosphate diphosphohydrolase8 | - |
Homo sapiens |
| 3.6.1.5 | NTPDase1 | - |
Homo sapiens |
| 3.6.1.5 | NTPDase2 | - |
Homo sapiens |
| 3.6.1.5 | NTPDase3 | - |
Homo sapiens |
| 3.6.1.5 | NTPDase8 | - |
Homo sapiens |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.6.1.5 | 0.0225 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase3 | Homo sapiens | |
| 3.6.1.5 | 0.0387 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase8 | Homo sapiens | |
| 3.6.1.5 | 0.0494 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase2 | Homo sapiens | |
| 3.6.1.5 | 0.119 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase1 | Homo sapiens | |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.6.1.5 | 6.5 | - |
assay at | Homo sapiens |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 3.6.1.5 | physiological function | ecto-nucleoside triphosphate diphosphohydrolase1 (NTPDase1, CD39) is a major ectonucleotidase that hydrolyzes proinflammatory ATP via ADP to AMP, which is subsequently converted by ecto-5'-nucleotidase (CD73) to immunosuppressive adenosine | Homo sapiens |
kcat/KM [mM/s]
| EC Number | kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.6.1.5 | 0.37 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase8 | Homo sapiens | |
| 3.6.1.5 | 0.89 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase2 | Homo sapiens | |
| 3.6.1.5 | 1.69 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase3 | Homo sapiens | |
| 3.6.1.5 | 6.07 | - |
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate | pH 6.5, temperature not specified in the publication, NTPDase1 | Homo sapiens | |
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