ArticleACS medicinal chemistry letters2012
β-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 37 citations in OpenAlex.
- Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-CovalentJournal of medicinal chemistry · 2021Article
- Synthesis, biological evaluation, and structure activity relationship (SAR) study of pyrrolidine amide derivatives asMedChemComm · 2019Article
- Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase.Journal of visualized experiments : JoVE · 2016Article
- Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis.Angewandte Chemie (International ed. in English) · 2016Article
- Activity-Based Probe for N-Acylethanolamine Acid Amidase.ACS chemical biology · 2015Article
- A Potent Systemically Active N-Acylethanolamine Acid Amidase Inhibitor that Suppresses Inflammation and Human Macrophage Activation.ACS chemical biology · 2015Article
- Advances in the discovery of N-acylethanolamine acid amidase inhibitors.Pharmacological research · 2014Review
- Peripheral gating of pain signals by endogenous lipid mediators.Nature neuroscience · 2014Review
- Article
- Peroxisome proliferator-activated receptor α mediates acute effects of palmitoylethanolamide on sensory neurons.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- Biochemical and mass spectrometric characterization of human N-acylethanolamine-hydrolyzing acid amidase inhibition.PloS one · 2012Article
Corrections and comments
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Authors and funding
14 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The cysteine amidase N-acylethanolamine acid amidase (NAAA) is a member of the N-terminal nucleophile class of enzymes and a potential target for anti-inflammatory drugs. We investigated the mechanism of inhibition of human NAAA by substituted β-lactones. We characterized pharmacologically a representative member of this class, ARN077, and showed, using high-resolution liquid chromatography-tandem mass spectrometry, that this compound forms a thioester bond with the N-terminal catalytic cysteine in human NAAA.
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