N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRβ

…, J Nabakka, F Liang, J Wityak, A Koder…

文献索引：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 Journal of Medicinal Chemistry, 2007 , vol. 50, # 17 p. 4255 - 4259

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被引用次数: 66

摘要

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 ...