2. Academic Validation
  3. Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)

Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)

  • Chem Commun (Camb). 2017 Nov 28;53(95):12814-12817. doi: 10.1039/c7cc07582k.
Beatrice Castellani 1,  Eleonora Diamanti,  Daniela Pizzirani,  Piero Tardia,  Martina Maccesi,  Natalia Realini,  Paola Magotti,  Gianpiero Garau,  Thomas Bakkum,  Silvia Rivara,  Marco Mor,  Daniele Piomelli
Affiliations

Affiliation

  • 1 Drug Discovery and Development, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
PMID: 29143042 DOI: 10.1039/c7cc07582k
Abstract

N-Acylphosphatidylethanolamine Phospholipase D (NAPE-PLD) is a membrane-associated zinc Enzyme that catalyzes the hydrolysis of N-acylphosphatidylethanolamines (NAPEs) into fatty acid ethanolamides (FAEs). Here, we describe the identification of the first small-molecule NAPE-PLD inhibitor, the quinazoline sulfonamide derivative 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide, ARN19874.

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