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Literature summary for 3.5.1.60 extracted from

  • West, J.M.; Zvonok, N.; Whitten, K.M.; Vadivel, S.K.; Bowman, A.L.; Makriyannis, A.
    Biochemical and mass spectrometric characterization of human N-acylethanolamine-hydrolyzing acid amidase inhibition (2012), PLoS ONE, 7, e43877.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of the C-terminally His6-tagged enzyme in HEK-293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-isothiocyanatopentadecane a potent, selective and reversible inhibitor Homo sapiens
5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide inhibits the enzyme in a covalent and irreversible manner Homo sapiens
additional information mechanism of inactivation of human enzyme N-acylethanolamine-hydrolyzing acid amidase with selected inhibitors identified in a fluorescent based assay developed for characterization of both reversible and irreversible inhibitors, kinetic analysis using MALDI-TOF mass spectroscopy, molecular modeling, overview Homo sapiens
N-benzyloxycarbonyl-L-serine beta-lactone inhibits the enzyme in a covalent and irreversible manner Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0062
-
N-(4-methylcoumarin)palmitamide recombinant enzyme, pH not specified in the publication, 37°C Homo sapiens
0.021
-
N-palmitoylethanolamine recombinant enzyme, pH not specified in the publication, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q02083
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant C-terminally His6-tagged enzyme from HEK-293 cells by nickel affinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-(4-methylcoumarin)palmitamide + H2O
-
Homo sapiens palmitic acid + 7-amino-4-methylcoumarin
-
?
N-palmitoylethanolamine + H2O
-
Homo sapiens palmitic acid + ethanolamine
-
?

Synonyms

Synonyms Comment Organism
N-acylethanolamine-hydrolyzing acid amidase
-
Homo sapiens

Temperature Optimum [°C]

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000013
-
5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide recombinant enzyme, pH not specified in the publication, 37°C Homo sapiens
0.0013
-
N-benzyloxycarbonyl-L-serine beta-lactone recombinant enzyme, pH not specified in the publication, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000072
-
recombinant enzyme with substrate N-palmitoylethanolamine, pH not specified in the publication, 37°C Homo sapiens 5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide
0.0000077
-
recombinant enzyme with substrate N-(4-methyl coumarin)palmitamide, pH not specified in the publication, 37°C Homo sapiens 5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide
0.00035
-
recombinant enzyme with substrate N-(4-methyl coumarin)palmitamide, pH not specified in the publication, 37°C Homo sapiens 1-isothiocyanatopentadecane
0.0006
-
recombinant enzyme with substrate N-palmitoylethanolamine, pH not specified in the publication, 37°C Homo sapiens 1-isothiocyanatopentadecane
0.0017
-
recombinant enzyme with substrate N-(4-methyl coumarin)palmitamide, pH not specified in the publication, 37°C Homo sapiens N-benzyloxycarbonyl-L-serine beta-lactone
0.0019
-
recombinant enzyme with substrate N-palmitoylethanolamine, pH not specified in the publication, 37°C Homo sapiens N-benzyloxycarbonyl-L-serine beta-lactone