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ID: ALA3259798

Journal: Bioorg Med Chem Lett

Title: A novel Lipoprotein lipase (LPL) agonist rescues the enzyme from inhibition by angiopoietin-like 4 (ANGPTL4).

Authors: Geldenhuys WJ, Aring D, Sadana P.

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.

CiteXplore: 24703657

DOI: 10.1016/j.bmcl.2014.03.021