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

Molteni, Valentina and Li, Xiaolin and Nabakka, Juliet and Liang, Fang and Wityak, John and Koder, Alan and Vargas, Leonardo and Romeo, Russell and Mitro, Nico and Mak, Pui Ying and Seidel, Martin and Haslam, Jennifer and Chow, Donald and Tuntland, Tove and Spalding, Tracy and Brock, Ansgar and Bradley, Michelle and Castrillo, Antonio and Tontonoz, Peter and Saez, Enrique (2007) N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. Journal of Medicinal Chemistry, 50 (17). pp. 4255-4259. ISSN 0022-2623

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.

Item Type: Article
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Date Deposited: 14 Dec 2009 14:05
Last Modified: 31 Jan 2013 01:27
URI: https://oak.novartis.com/id/eprint/111

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