| Literature DB >> 24703657 |
Werner J Geldenhuys1, Danielle Aring1, Prabodh Sadana2.
Abstract
Lipoprotein lipase (LPL) is a key physiological regulator of triglycerides and atherosclerosis risk. Random screening identified a compound designated C10, showing greater LPL agonist activity than NO-1886, a known LPL agonist. Structure-activity relationship (SAR) exploration of C10 led to the identification of C10d exhibiting at least two fold greater LPL activation than NO-1886. Unlike NO-1886, novel LPL agonists C10 and C10d reversed the LPL inhibition by angiopoietin-like 4 (ANGPTL4), a physiological inhibitor of LPL.Entities:
Keywords: ANGPTL4; Atherosclerosis; High-throughput screen; Homology model; Ibrolipim; LPL; NO-1886
Mesh：
Substances：
Year: 2014 PMID： 24703657 DOI： 10.1016/j.bmcl.2014.03.021
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823