| Literature DB >> 17665897 |
Valentina Molteni1, Xiaolin Li, Juliet Nabakka, Fang Liang, John Wityak, Alan Koder, Leo Vargas, Russell Romeo, Nico Mitro, Puiying A Mak, H Martin Seidel, Jennifer A Haslam, Donald Chow, Tove Tuntland, Tracy A Spalding, Ansgar Brock, Michelle Bradley, Antonio Castrillo, Peter Tontonoz, Enrique Saez.
Abstract
We have identified a novel liver X receptor (LXR) agonist (2) that activates the LXRbeta subtype with selectivity over LXRalpha. LXRbeta 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 LXRbeta selectivity in a small molecule while maintaining functional LXR activity.Entities:
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Year: 2007 PMID： 17665897 DOI： 10.1021/jm070453f
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446