Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD).
| Title | Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD). |
| Publication Type | Journal Article |
| Year of Publication | 2017 |
| Authors | Castellani, B., Diamanti E., Pizzirani D., Tardia P., Maccesi M., Realini N., Magotti P., Garau G., Bakkum T., Rivara S., Mor M., & Piomelli D. |
| Journal | Chem Commun (Camb) |
| Volume | 53 |
| Issue | 95 |
| Pagination | 12814-12817 |
| Date Published | 2017 Nov 28 |
| ISSN | 1364-548X |
| Keywords | Dose-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. |
| DOI | 10.1039/c7cc07582k |
| Alternate Journal | Chem. Commun. (Camb.) |
| PubMed ID | 29143042 |
| PubMed Central ID | PMC5730275 |
| Grant List | R01 DA012413 / DA / NIDA NIH HHS / United States |
