Petracca Rita, Romeo Elisa, Baggelaar Marc P, Artola Marta, Pontis Silvia, Ponzano Stefano, Overkleeft Herman S, van der Stelt Mario, Piomelli Daniele
School of Chemistry and Trinity Biomedical Sciences Institute (TBSI), Trinity College Dublin, The University of Dublin, Dublin 2, Ireland.
Chem Commun (Camb). 2017 Aug 22;53(86):11810-11813. doi: 10.1039/c7cc06838g.
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.
半胱氨酸水解酶N-酰基乙醇胺酸酰胺酶(NAAA)是一种很有前景的镇痛和抗炎药物靶点。在此,我们描述了两种前所未有的基于NAAA反应活性的探针的开发,作为研究工具,用于发现新抑制剂以及在细胞环境中深入表征NAAA。