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.
MeSH terms
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Models, Molecular
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Molecular Structure
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Phospholipase D / antagonists & inhibitors*
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Phospholipase D / metabolism
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Quinazolines / chemical synthesis*
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Quinazolines / chemistry
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Quinazolines / pharmacology*
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Quinazolinones
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Small Molecule Libraries / chemical synthesis
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
Substances
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2,4-dioxo-N-(4-(4-pyridyl)phenyl)-1H-quinazoline-6-sulfonamide
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Enzyme Inhibitors
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Quinazolines
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Quinazolinones
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Small Molecule Libraries
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Sulfonamides
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Phospholipase D
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NAPEPLD protein, human