The english version of the website of the School of Medicine is under development

Δημοσίευση

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

TitleSynthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD).
Publication TypeJournal Article
Year of Publication2017
AuthorsCastellani, B., Diamanti E., Pizzirani D., Tardia P., Maccesi M., Realini N., Magotti P., Garau G., Bakkum T., Rivara S., Mor M., & Piomelli D.
JournalChem Commun (Camb)
Volume53
Issue95
Pagination12814-12817
Date Published2017 Nov 28
ISSN1364-548X
KeywordsDose-Response Relationship, Drug, Enzyme Inhibitors, Humans, Models, Molecular, Molecular Structure, Phospholipase D, Quinazolines, Quinazolinones, Small Molecule Libraries, Structure-Activity Relationship, Sulfonamides
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.

DOI10.1039/c7cc07582k
Alternate JournalChem. Commun. (Camb.)
PubMed ID29143042
PubMed Central IDPMC5730275
Grant ListR01 DA012413 / DA / NIDA NIH HHS / United States

Contact

Secretariat of the School of Medicine
 

Connect

Schoole of Medicince presence in social networks
Follow Us or Connect with us.