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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| Veröffentlicht in: | Journal of medicinal chemistry 2007-08, Vol.50 (17), p.4255-4259 |
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| container_issue | 17 |
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| container_title | Journal of medicinal chemistry |
| container_volume | 50 |
| creator | 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 |
| description | 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. |
| doi_str_mv | 10.1021/jm070453f |
| format | Article |
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| source | ACS Publications |
| subjects | Biological and medical sciences Hormones. Endocrine system Medical sciences Pharmacology. Drug treatments |
| title | N-Acylthiadiazolines, a New Class of Liver X Receptor Agonists with Selectivity for LXRβ |
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