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Synthesis and characterization of the first inhibitor of N -acylphosphatidylethanolamine phospholipase D (NAPE-PLD)
- Castellani, Beatrice;
- Diamanti, Eleonora;
- Pizzirani, Daniela;
- Tardia, Piero;
- Maccesi, Martina;
- Realini, Natalia;
- Magotti, Paola;
- Garau, Gianpiero;
- Bakkum, Thomas;
- Rivara, Silvia;
- Mor, Marco;
- Piomelli, Daniele
Published Web Location
https://doi.org/10.1039/c7cc07582kAbstract
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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