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Literature summary for 3.6.1.5 extracted from
- Fluorescence polarization immunoassays for monitoring nucleoside triphosphate diphosphohydrolase (NTPDase) activity (2015), Analyst, 140, 140-148 .
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | the NTPDase isozymes are targets for development of potent and selective drug-like NTPDase inhibitors | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression of the isozyme in COS-7 cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-amino-4-[(naphthalen-1-yl)amino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid | PSB-06126, an anthraquinone derivative, competitive mechanism of inhibition | Homo sapiens |  |
| additional information | identification of subtype-selective inhibitors, and development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout, for inhibitor screening. Methods comparisons, overview. The evaluated methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1); identification of subtype-selective inhibitors, and development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout, for inhibitor screening. Methods comparisons, overview. The evaluated methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1); identification of subtype-selective inhibitors, and development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout, for inhibitor screening. Methods comparisons, overview. The evaluated methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1); identification of subtype-selective inhibitors, and development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout, for inhibitor screening. Methods comparisons, overview. The evaluated methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1) | 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 | |
| 0.017 | - |
ATP | pH 7.5, 37°C, recombinant enzyme | Homo sapiens | |
| 0.07 | - |
ATP | pH 7.5, 37°C, recombinant enzyme | Homo sapiens | |
| 0.075 | - |
ATP | pH 7.5, 37°C, recombinant enzyme | Homo sapiens | |
| 0.081 | 0.226 | ATP | pH 7.5, 37°C, recombinant enzyme | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | - |
Homo sapiens | 16020 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | Homo sapiens | |
| Mg2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ADP + H2O | Homo sapiens | - |
AMP + phosphate | - |
? | |
| ADP + H2O | Homo sapiens | very low activity | AMP + phosphate | - |
? | |
| ATP + 2 H2O | Homo sapiens | ATP is hydrolyzed by NTPDase1 via ADP to AMP, without significant release of ADP | AMP + 2 phosphate | - |
ir | |
| ATP + H2O | Homo sapiens | - |
ADP + phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O75355 | - |
- |
| Homo sapiens | P49961 | - |
- |
| Homo sapiens | Q5MY95 | - |
- |
| Homo sapiens | Q9Y5L3 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ADP + H2O | - |
Homo sapiens | AMP + phosphate | - |
? | |
| ADP + H2O | very low activity | Homo sapiens | AMP + phosphate | - |
? | |
| ATP + 2 H2O | ATP is hydrolyzed by NTPDase1 via ADP to AMP, without significant release of ADP | Homo sapiens | AMP + 2 phosphate | - |
ir | |
| ATP + H2O | - |
Homo sapiens | ADP + phosphate | - |
? | |
| additional information | development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout. The methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1), evaluation and validation, overview | Homo sapiens | ? | - |
- |
|
| additional information | isozymes NTPDase2 hydrolyzes ATP to ADP, which is released from the enzyme. NTPDase2 shows much higher preference for ATP over ADP, and therefore produces ADP as its main product. Development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout. The methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1), evaluation and validation, overview | Homo sapiens | ? | - |
- |
|
| additional information | isozymes NTPDase3 and -8 hydrolyze ATP to ADP, which is released from the enzyme, and ADP is subsequently hydrolyzed to AMP. Development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrat, with fluorescence polarization (FP) readout. The methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1), evaluation and validation, overview | Homo sapiens | ? | - |
- |
|
| additional information | isozymes NTPDase3 and -8 hydrolyze ATP to ADP, which is released from the enzyme, and ADP is subsequently hydrolyzed to AMP. Development of a sensitive, reproducible method, a fluorescence polarization immunoassay, which allows the detection of NTPDase activity with its natural substrate, with fluorescence polarization (FP) readout. The methodology is generally applicable for ADP-, AMP- or GMP-producing enzymes. It enables the direct detection of the enzymatic reaction product ADP when using ATP as a substrate (for NTPDase2, NTPDase3, and NTPDase8) or of AMP upon using ADP as a substrate (for NTPDase1), evaluation and validation, overview | Homo sapiens | ? | - |
- |
|
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| NTPDase | - |
Homo sapiens |
| NTPDase1 | - |
Homo sapiens |
| NTPDase2 | - |
Homo sapiens |
| NTPDase3 | - |
Homo sapiens |
| nucleoside triphosphate diphosphohydrolase | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00439 | - |
1-amino-4-[(naphthalen-1-yl)amino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid | pH 7.5, 37°C, recombinant enzyme | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00776 | - |
pH 7.5, 37°C, recombinant enzyme | Homo sapiens | 1-amino-4-[(naphthalen-1-yl)amino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonic acid | |
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