The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages |
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| Authors: | Joseph P. Marino Lara S. Kallander Chun Ma Hye-Ja Oh Dennis Lee Dimitri E. Gaitanopoulos John A. Krawiec Derek J. Parks Christine L. Webb Kelly Ziegler Michael Jaye Scott K. Thompson |
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| Affiliation: | 1. Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, United States;2. Biology, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, United States;3. Biochemical and Cellular Targets, Molecular Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, United States |
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| Abstract: | ![]()
The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism. SAR studies around tertiary-amine lead molecule 2, an LXR full agonist, revealed that steric and conformational changes to the acetic acid and propanolamine groups produce dramatic effects on agonist efficacy and potency. The new analogs possess good functional activity, demonstrating the ability to upregulate LXR target genes, as well as promote cholesterol efflux in macrophages. |
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