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Literature summary extracted from

  • Ribeiro, A.; Pontis, S.; Mengatto, L.; Armirotti, A.; Chiurchiu, V.; Capurro, V.; Fiasella, A.; Nuzzi, A.; Romeo, E.; Moreno-Sanz, G.; Maccarrone, M.; Reggiani, A.; Tarzia, G.; Mor, M.; Bertozzi, F.; Bandiera, T.; Piomelli, D.
    A potent systemically active N-acylethanolamine acid amidase inhibitor that suppresses inflammation and human macrophage activation (2015), ACS Chem. Biol., 10, 1838-1846 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.5.1.60 gene Naaa, recombinant expression in HEK-293 cells Homo sapiens
3.5.1.60 gene Naaa, stable transfection and functional recombinant expression in HEK-293 cells Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.1.60 4-cyclohexylbutyl-N-[(R)-2-oxoazetidin-3-yl]carbamate
-
 Homo sapiens
3.5.1.60 4-cyclohexylbutyl-N-[(R)-2-oxoazetidin-3-yl]carbamate
-
 Mus musculus
3.5.1.60 4-cyclohexylbutyl-N-[(R)-2-oxoazetidin-3-yl]carbamate
-
 Rattus norvegicus
3.5.1.60 4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate it blocks enzyme NAAA by covalently binding to the enzyme's catalytic cysteine and displays pronounced antiinflammatory properties in human macrophages Homo sapiens
3.5.1.60 4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate the compound is quickly eliminated in vivo. It blocks enzyme NAAA by covalently binding to the enzyme's catalytic cysteine and displays pronounced antiinflammatory properties in mouse models Mus musculus
3.5.1.60 4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate the compound is quickly eliminated in vivo Rattus norvegicus
3.5.1.60 5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate
-
 Homo sapiens
3.5.1.60 5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate
-
 Mus musculus
3.5.1.60 5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate
-
 Rattus norvegicus
3.5.1.60 additional information inhibitor desing and synthesis of a class of beta-lactam derivatives that are potent, selective, and systemically active inhibitors of intracellular NAAA activity, reaction mechanisms via acylation or alkylation of the enzyme, overview Homo sapiens
3.5.1.60 additional information inhibitor desing and synthesis of a class of beta-lactam derivatives that are potent, selective, and systemically active inhibitors of intracellular NAAA activity, reaction mechanisms via acylation or alkylation of the enzyme, overview Mus musculus
3.5.1.60 additional information inhibitor desing and synthesis of a class of beta-lactam derivatives that are potent, selective, and systemically active inhibitors of intracellular NAAA activity, reaction mechanisms via acylation or alkylation of the enzyme, overview Rattus norvegicus
3.5.1.60 N-[(3S)-2-oxoazetidin-3-yl]nonanamide
-
 Homo sapiens
3.5.1.60 N-[(3S)-2-oxoazetidin-3-yl]nonanamide
-
 Mus musculus
3.5.1.60 N-[(3S)-2-oxoazetidin-3-yl]nonanamide
-
 Rattus norvegicus
3.5.1.60 N-[(3S)-2-oxooxetan-3-yl]-3-phenylpropanamide
-
 Homo sapiens
3.5.1.60 N-[(3S)-2-oxooxetan-3-yl]-3-phenylpropanamide
-
 Mus musculus
3.5.1.60 N-[(3S)-2-oxooxetan-3-yl]-3-phenylpropanamide
-
 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.5.1.60 lysosome
-
 Homo sapiens 5764
-
3.5.1.60 lysosome
-
 Rattus norvegicus 5764
-
3.5.1.60 lysosome
-
 Mus musculus 5764
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.5.1.60 oleoylethanolamide + H2O Homo sapiens
-
 oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O Rattus norvegicus
-
 oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O Mus musculus
-
 oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O Mus musculus C57BL/6J
-
 oleate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O Homo sapiens
-
 palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O Rattus norvegicus
-
 palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O Mus musculus
-
 palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O Mus musculus C57BL/6J
-
 palmitate + ethanolamine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.5.1.60 Homo sapiens Q02083
-
-
3.5.1.60 Mus musculus Q9D7V9
-
-
3.5.1.60 Mus musculus C57BL/6J Q9D7V9
-
-
3.5.1.60 Rattus norvegicus Q5KTC7
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.5.1.60 lung
-
 Rattus norvegicus
-
3.5.1.60 lung
-
 Mus musculus
-
3.5.1.60 macrophage
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.5.1.60 oleoylethanolamide + H2O
-
 Homo sapiens oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O
-
 Rattus norvegicus oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O
-
 Mus musculus oleate + ethanolamine
-
 ?
3.5.1.60 oleoylethanolamide + H2O
-
 Mus musculus C57BL/6J oleate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O
-
 Homo sapiens palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O
-
 Rattus norvegicus palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O
-
 Mus musculus palmitate + ethanolamine
-
 ?
3.5.1.60 palmitoylethanolamide + H2O
-
 Mus musculus C57BL/6J palmitate + ethanolamine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.5.1.60 N-acylethanolamine acid amidase
-
 Homo sapiens
3.5.1.60 N-acylethanolamine acid amidase
-
 Rattus norvegicus
3.5.1.60 N-acylethanolamine acid amidase
-
 Mus musculus
3.5.1.60 NAAA
-
 Homo sapiens
3.5.1.60 NAAA
-
 Rattus norvegicus
3.5.1.60 NAAA
-
 Mus musculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.1.60 37
-
 assay at Homo sapiens
3.5.1.60 37
-
 assay at Rattus norvegicus
3.5.1.60 37
-
 assay at Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.5.1.60 8
-
 assay at Homo sapiens
3.5.1.60 8
-
 assay at Rattus norvegicus
3.5.1.60 8
-
 assay at Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.5.1.60 additional information
-
 additional information inhibition kinetic analysis Homo sapiens