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Literature summary for 3.5.1.60 extracted from

  • Romeo, E.; Ponzano, S.; Armirotti, A.; Summa, M.; Bertozzi, F.; Garau, G.; Bandiera, T.; Piomelli, D.
    Activity-based probe for N-acylethanolamine acid amidase (2015), ACS Chem. Biol., 10, 2057-2064 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.60

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate ARN726, the enzyme inhibitor exerts systemic anti-inflammatory effects in mouse models of lung inflammation Homo sapiens
4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate ARN726, the enzyme inhibitor exerts systemic anti-inflammatory effects in mouse models of lung inflammation Rattus norvegicus
5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate ARN077, the enzyme inhibitor is active in vivo by topical administration in rodent models of hyperalgesia and allodynia Homo sapiens
5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate ARN077, the enzyme inhibitor is active in vivo by topical administration in rodent models of hyperalgesia and allodynia Rattus norvegicus
additional information inhibitor binding analysis using purified and activated human enzyme hNAAA coupled to an azide-PEG3-biotin conjugate to its terminal alkyne using click chemistry, and visualization of protein bands using streptavidin-horseradish peroxidase (HRP) Homo sapiens
undec-10-ynyl N-[(3S)-2-oxoazetidin-3-yl]carbamate ARN14686, design and validation of this derivative of ARN726 as activity-based protein profiling (ABPP) probe for the in vivo detection of NAAA Rattus norvegicus
undec-10-ynyl-N-[(3S)-2-oxoazetidin-3-yl]carbamate ARN14686, design and validation of this derivative of ARN726 as activity-based protein profiling (ABPP) probe for the in vivo detection of NAAA Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-
lysosome
-
 Rattus norvegicus 5764
-
additional information subcellular localization study Rattus norvegicus
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q02083
-
-
Rattus norvegicus Q5KTC7
-
-
Rattus norvegicus Sprague-Dawley Q5KTC7
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lung high enzyme content Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
N-acylethanolamine acid amidase
-
 Homo sapiens
N-acylethanolamine acid amidase
-
 Rattus norvegicus
NAAA
-
 Homo sapiens
NAAA
-
 Rattus norvegicus

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
4.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
 pH and temperature not specified in the publication Homo sapiens undec-10-ynyl-N-[(3S)-2-oxoazetidin-3-yl]carbamate
0.000007
-
 pH and temperature not specified in the publication Homo sapiens 5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate
0.000013
-
 pH and temperature not specified in the publication Rattus norvegicus undec-10-ynyl N-[(3S)-2-oxoazetidin-3-yl]carbamate
0.000027
-
 pH and temperature not specified in the publication Homo sapiens 4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate
0.00005
-
 pH and temperature not specified in the publication Rattus norvegicus 5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate
0.000063
-
 pH and temperature not specified in the publication Rattus norvegicus 4-cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate

General Information

General Information Comment Organism
physiological function N-acylethanolamine acid amidase (NAAA) is a lysosomal cysteine hydrolase involved in the degradation of saturated and monounsaturated fatty acid ethanolamides (FAEs), a family of endogenous lipid signaling molecules that includes oleoylethanolamide (OEA) and palmitoylethanolamide (PEA) Homo sapiens
physiological function N-acylethanolamine acid amidase (NAAA) is a lysosomal cysteine hydrolase involved in the degradation of saturated and monounsaturated fatty acid ethanolamides (FAEs), a family of endogenous lipid signaling molecules that includes oleoylethanolamide (OEA) and palmitoylethanolamide (PEA) Rattus norvegicus