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Article
Peer Reviewed

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

UC Irvine Previously Published Works (2017)

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.

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