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Issue 95, 2017
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Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)

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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.

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

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Publication details

The article was received on 30 Sep 2017, accepted on 06 Nov 2017 and first published on 16 Nov 2017


Article type: Communication
DOI: 10.1039/C7CC07582K
Citation: Chem. Commun., 2017,53, 12814-12817
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    Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)

    B. Castellani, E. Diamanti, D. Pizzirani, P. Tardia, M. Maccesi, N. Realini, P. Magotti, G. Garau, T. Bakkum, S. Rivara, M. Mor and D. Piomelli, Chem. Commun., 2017, 53, 12814
    DOI: 10.1039/C7CC07582K

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