Novel activity-based probes for N-acylethanolamine acid amidase

Chem Commun (Camb). 2017 Aug 22;53(86):11810-11813. doi: 10.1039/c7cc06838g.

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.

MeSH terms

  • Amidohydrolases / antagonists & inhibitors
  • Amidohydrolases / metabolism*
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Molecular Probes / chemical synthesis
  • Molecular Probes / chemistry*
  • Molecular Probes / metabolism*
  • Molecular Structure
  • Threonine / chemistry
  • beta-Lactams / chemistry

Substances

  • Enzyme Inhibitors
  • Molecular Probes
  • beta-Lactams
  • Threonine
  • Amidohydrolases
  • NAAA protein, human