A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.
Bioorg Med Chem Lett
; 23(9): 2595-7, 2013 May 01.
Article
em En
| MEDLINE
| ID: mdl-23528297
ABSTRACT
By screening directed libraries of serine hydrolase inhibitors using the cell surface form of endothelial lipase (EL), we identified a series of carbamate-derived (EL) inhibitors. Compound 3 raised plasma HDL-C levels in the mouse, and a correlation was found between HDL-C and plasma compound levels. Spectroscopic and kinetic studies support a covalent mechanism of inhibition. Our findings represent the first report of EL inhibition as an effective means for increasing HDL-C in an in vivo model.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiocarbamatos
/
Endotélio Vascular
/
Inibidores Enzimáticos
/
Lipase
/
HDL-Colesterol
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article