Geldenhuys_2014_Bioorg.Med.Chem.Lett_24_2163

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.