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N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta |
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| 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 |
| Affiliation: | Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, USA. vmolteni@gnf.org |
| 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. |
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