PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor

[Image: see text] Screening of a small set of nonselective lipase inhibitors against endothelial lipase (EL) identified a potent and reversible inhibitor, N-(3-(3,4-dichlorophenyl)propyl)-3-hydroxy-1-methyl-2-oxo-1,2-dihydropyridine-4-carboxamide (5; EL IC(50) = 61 nM, EL(HDL) IC(50) = 454 nM). Deck...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Hangeland, Jon J., Abell, Lynn M., Adam, Leonard P., Jiang, Ji, Friends, Todd J., Haque, Lauren E., Neels, James, Onorato, Joelle M., Chen, Alice Ye A., Taylor, David S., Yin, Xiaohong, Harrity, Thomas W., Basso, Michael D., Yang, Richard, Sleph, Paul G., Gordon, David A., Huang, Christine S., Wexler, Ruth R., Finlay, Heather J., Lawrence, R. Michael
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6047032/
https://ncbi.nlm.nih.gov/pubmed/30034599
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00138
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