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

Title

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

Creator

Geldenhuys Werner J; Aring Danielle; Sadana Prabodh

Publisher

Bioorganic & medicinal chemistry letters

Date

2014
2014-05

Description

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

Subject

Angiopoietin-like 4 Protein; Angiopoietins/*metabolism; ANGPTL4; Atherosclerosis; Benzamides/pharmacology; Drug Discovery; Enzyme Activation/*drug effects; High-throughput screen; Homology model; Humans; Ibrolipim; Lipoprotein Lipase/*metabolism; LPL; Molecular Docking Simulation; NO-1886; Organophosphorus Compounds/pharmacology

Rights

Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).

URL Address

http://doi.org/10.1016/j.bmcl.2014.03.021

Pages

2163–2167

Issue

9

Volume

24

Citation

Geldenhuys Werner J; Aring Danielle; Sadana Prabodh, “A novel Lipoprotein lipase (LPL) agonist rescues the enzyme from inhibition by angiopoietin-like 4 (ANGPTL4).,” NEOMED Bibliography Database, accessed April 27, 2024, https://neomed.omeka.net/items/show/3500.