N-Acylthiadiazolines, a New Class of Liver X Receptor Agonists with Selectivity for LXRβ

We have identified a novel liver X receptor (LXR) agonist (2) that activates the LXRβ subtype with selectivity over LXRα. LXRβ selectivity was confirmed using macrophages derived from LXR mutant mice. Despite its selectivity and modest potency, the compound can induce APO-AI-dependent cholesterol ef...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2007-08, Vol.50 (17), p.4255-4259
Main Authors: Molteni, Valentina, Li, Xiaolin, Nabakka, Juliet, Liang, Fang, Wityak, John, Koder, Alan, Vargas, Leo, Romeo, Russell, Mitro, Nico, Mak, Puiying A, Seidel, H. Martin, Haslam, Jennifer A, Chow, Donald, Tuntland, Tove, Spalding, Tracy A, Brock, Ansgar, Bradley, Michelle, Castrillo, Antonio, Tontonoz, Peter, Saez, Enrique
Format: Article
Language:English
Subjects:
Biological and medical sciences
Hormones. Endocrine system
Medical sciences
Pharmacology. Drug treatments
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Summary:We have identified a novel liver X receptor (LXR) agonist (2) that activates the LXRβ subtype with selectivity over LXRα. LXRβ selectivity was confirmed using macrophages derived from LXR mutant mice. Despite its selectivity and modest potency, the compound can induce APO-AI-dependent cholesterol efflux from macrophages with full efficacy. Our results indicate that it is possible to achieve significant LXRβ selectivity in a small molecule while maintaining functional LXR activity.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm070453f