Novel activity-based probes for N-acylethanolamine acid amidase

Rita Petracca; Elisa Romeo; Marc P. Baggelaar; Marta Artola; Silvia Pontis; Stefano Ponzano; Herman S. Overkleeft; Mario van der Stelt; Daniele Piomelli

doi:10.1039/C7CC06838G

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Novel activity-based probes for N-acylethanolamine acid amidase†

Rita Petracca,

‡^ab Elisa Romeo,

‡^b Marc P. Baggelaar,

^c Marta Artola,

^d Silvia Pontis,

^b Stefano Ponzano,

^b Herman S. Overkleeft,

^d Mario van der Stelt

^c and Daniele Piomelli

*^e

Author affiliations

* Corresponding authors

^a School of Chemistry and Trinity Biomedical Sciences Institute (TBSI), Trinity College Dublin, The University of Dublin, Dublin 2, Ireland

^b Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, Italy

^c Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, The Netherlands

^d Department of Bio-organic Synthesis, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden, The Netherlands

^e Departments of Anatomy and Neurobiology, Pharmacology and Biological Chemistry, University of California, Irvine, USA
E-mail: piomelli@uci.edu

Abstract

The cysteine hydrolase, N-acylethanolamine acid amidase (NAAA) is a promising target for analgesic and anti-inflammatory drugs. Here, we describe the development of two unprecedented NAAA-reactive activity-based probes as research tools for application in the discovery of new inhibitors and for the in-depth characterization of NAAA in its cellular environment.

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Article information

DOI: https://doi.org/10.1039/C7CC06838G
Article type: Communication
Submitted: 31 Aug 2017
Accepted: 09 Oct 2017
First published: 10 Oct 2017

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Chem. Commun., 2017,53, 11810-11813

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Novel activity-based probes for N-acylethanolamine acid amidase

R. Petracca, E. Romeo, M. P. Baggelaar, M. Artola, S. Pontis, S. Ponzano, H. S. Overkleeft, M. van der Stelt and D. Piomelli, Chem. Commun., 2017, 53, 11810 DOI: 10.1039/C7CC06838G

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Chemical Communications

Novel activity-based probes for N-acylethanolamine acid amidase†

Abstract

Supplementary files

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Novel activity-based probes for N-acylethanolamine acid amidase

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