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Literature summary for 3.5.1.60 extracted from
- Development of new inhibitors for N-acylethanolamine-hydrolyzing acid amidase as promising tool against bladder cancer (2017), Bioorg. Med. Chem., 25, 1242-1249 .
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | inhibitors against N-acylethanolamine-hydrolyzing acid amidase are promising tools against bladder cancer | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (2R)-2-hydroxy-N-pentadecyl-2-phenylacetamide | - |
Homo sapiens |  |
| (2S)-2-hydroxy-N-pentadecyl-2-phenylacetamide | - |
Homo sapiens | |
| 2,5-dihydroxy-N-pentadecylbenzamide | - |
Homo sapiens | |
| 2-hydroxy-N-pentadecylbenzamide | - |
Homo sapiens | |
| additional information | identification of N-acylethanolamine-hydrolyzing acid amidase inhibitors able to reduce cell proliferation and migration and cause cell death on different bladder cancer cell lines. Inhibitor design of NAAA palmitic acid-retroamide inhibitors, synthesis, and characterization. Fluorescence high-throughput screening method set-up on human recombinant NAAA, using non-fluorescent but fluorogenic N-(4-methylcoumarin)palmitamide (PAMCA), that also allows to characterize the mechanism of inhibition. Reversibility of the inhibition. The NAAA inhibitors affect bladder cancer cells viability, they can be effective in inducing tumor cell death. But the inhibitors are differently effective of the different cell lines, overview | Homo sapiens | |
| N-pentadecylbenzamide | - |
Homo sapiens | |
| N-pentadecylbutanamide | - |
Homo sapiens | |
| N-pentadecylnaphthalene-2-carboxamide | - |
Homo sapiens | |
| N-pentadecylpyridine-4-carboxamide | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| lysosome | - |
Homo sapiens | 5764 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| N-alpha-linolenoylethanolamide + H2O | Homo sapiens | - |
alpha-linoleate + ethanolamine | - |
? | |
| N-arachidonoylethanolamide + H2O | Homo sapiens | - |
arachidonate + ethanolamine | - |
? | |
| N-eicosapentaenoylethanolamide + H2O | Homo sapiens | - |
eicosapentanoate + ethanolamine | - |
? | |
| N-linoleoylethanolamide + H2O | Homo sapiens | - |
linoleate + ethanolamine | - |
? | |
| N-oleoylethanolamide + H2O | Homo sapiens | - |
oleate + ethanolamine | - |
? | |
| N-palmitoylethanolamide + H2O | Homo sapiens | - |
palmitate + ethanolamine | - |
? | |
| N-stearoylethanolamide + H2O | Homo sapiens | - |
stearate + ethanolamine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q02083 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| 5637 cell | - |
Homo sapiens | - |
| bladder | - |
Homo sapiens | - |
| bladder transitional cell carcinoma cell | - |
Homo sapiens | - |
| HT-1376 cell | - |
Homo sapiens | - |
| RT-112 cell | - |
Homo sapiens | - |
| RT-4 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| N-alpha-linolenoylethanolamide + H2O | - |
Homo sapiens | alpha-linoleate + ethanolamine | - |
? | |
| N-arachidonoylethanolamide + H2O | - |
Homo sapiens | arachidonate + ethanolamine | - |
? | |
| N-eicosapentaenoylethanolamide + H2O | - |
Homo sapiens | eicosapentanoate + ethanolamine | - |
? | |
| N-linoleoylethanolamide + H2O | - |
Homo sapiens | linoleate + ethanolamine | - |
? | |
| N-oleoylethanolamide + H2O | - |
Homo sapiens | oleate + ethanolamine | - |
? | |
| N-palmitoylethanolamide + H2O | - |
Homo sapiens | palmitate + ethanolamine | - |
? | |
| N-stearoylethanolamide + H2O | - |
Homo sapiens | stearate + ethanolamine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| N-acylethanolamine-hydrolyzing acid amidase | - |
Homo sapiens |
| NAAA | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.011 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-hydroxy-N-pentadecylbenzamide | |
| 0.02 | - |
pH and temperature not specified in the publication | Homo sapiens | (2R)-2-hydroxy-N-pentadecyl-2-phenylacetamide | |
| 0.034 | - |
pH and temperature not specified in the publication | Homo sapiens | N-pentadecylbutanamide | |
| 0.038 | - |
pH and temperature not specified in the publication | Homo sapiens | 2,5-dihydroxy-N-pentadecylbenzamide | |
| 0.045 | - |
pH and temperature not specified in the publication | Homo sapiens | N-pentadecylbenzamide | |
| 0.078 | - |
pH and temperature not specified in the publication | Homo sapiens | (2S)-2-hydroxy-N-pentadecyl-2-phenylacetamide | |
| 0.098 | - |
pH and temperature not specified in the publication | Homo sapiens | N-pentadecylpyridine-4-carboxamide | |
| 0.1 | - |
above, pH and temperature not specified in the publication | Homo sapiens | N-pentadecylnaphthalene-2-carboxamide | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | important role for NAAA in cell migration and in inducing tumor cell death promoting this enzyme as pharmacological target against bladder cancer | Homo sapiens |
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