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Bioorg Med Chem Lett. 2013 May 1;23(9):2595-7. doi: 10.1016/j.bmcl.2013.02.113. Epub 2013 Mar 7.

A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.

Author information

1
Janssen Research and Development, LLC, Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, USA. grecom97@gmail.com

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.

PMID:
23528297
DOI:
10.1016/j.bmcl.2013.02.113
[Indexed for MEDLINE]

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