| Title : A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice - Greco_2013_Bioorg.Med.Chem.Lett_23_2595 |
| Author(s) : Greco MN , Connelly MA , Leo GC , Olson MW , Powell E , Huang Z , Hawkins M , Smith C , Schalk-Hihi C , Darrow AL , Xin H , Lang W , Damiano BP , Hlasta DJ |
| Ref : Bioorganic & Medicinal Chemistry Lett , 23 :2595 , 2013 |
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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. |
| PubMedSearch : Greco_2013_Bioorg.Med.Chem.Lett_23_2595 |
| PubMedID: 23528297 |
Greco MN, Connelly MA, Leo GC, Olson MW, Powell E, Huang Z, Hawkins M, Smith C, Schalk-Hihi C, Darrow AL, Xin H, Lang W, Damiano BP, Hlasta DJ (2013)
A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice
Bioorganic & Medicinal Chemistry Lett
23 :2595
Greco MN, Connelly MA, Leo GC, Olson MW, Powell E, Huang Z, Hawkins M, Smith C, Schalk-Hihi C, Darrow AL, Xin H, Lang W, Damiano BP, Hlasta DJ (2013)
Bioorganic & Medicinal Chemistry Lett
23 :2595