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Literature summary for 3.5.1.60 extracted from

  • Sasso, O.; Summa, M.; Armirotti, A.; Pontis, S.; De Mei, C.; Piomelli, D.
    The N-Acylethanolamine acid amidase inhibitor ARN077 suppresses inflammation and pruritus in a mouse model of allergic dermatitis (2018), J. Invest. Dermatol., 138, 562-569 .
    View publication on PubMed

Application

Application Comment Organism
drug development NAAA is a promising target for the development of effective and safe treatments for atopic dermatitis and other inflammatory disorders of the skin Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
5-phenylpentyl-N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]carbamate ARN077, a beta-lactone-based NAAA inhibitor that is rapidly deactivated in blood and other tissues. Analysis of properties of the NAAA inhibitor in a mouse model of allergic contact dermatitis. ARN077 suppresses DNFB-induced inflammation when administered either before or after the DNFB challenge. The effects of subchronic ARN077 are dose-dependent and comparable in size to those produced by the steroids clobetasol and dexamethasone. Unlike the latter, ARN077 does not cause skin atrophy Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
Mus musculus 5764
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
N-palmitoylethanolamide + H2O Mus musculus
-
palmitate + ethanolamine
-
?
N-palmitoylethanolamide + H2O Mus musculus CD-1
-
palmitate + ethanolamine
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-
Mus musculus CD-1
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
B-lymphocyte
-
Mus musculus
-
macrophage
-
Mus musculus
-
skin
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-palmitoylethanolamide + H2O
-
Mus musculus palmitate + ethanolamine
-
?
N-palmitoylethanolamide + H2O
-
Mus musculus CD-1 palmitate + ethanolamine
-
?

Synonyms

Synonyms Comment Organism
N-acylethanolamine acid amidase
-
Mus musculus
NAAA
-
Mus musculus

General Information

General Information Comment Organism
malfunction N-acylethanolamine acid amidase inhibitor ARN077 suppresses inflammation and pruritus in a mouse model of allergic dermatitis Mus musculus
physiological function N-acylethanolamine acid amidase (NAAA), a cysteine hydrolase that catalyzes the degradation of palmitoylethanolamide. Palmitoylethanolamide is an agonist of PPAR-alpha and an important regulator of pain and innate immunity Mus musculus