N-Acylthiadiazolines, a New Class of Liver X Receptor Agonists with Selectivity for LXRβ

Valentina Molteni; Xiaolin Li; Juliet Nabakka; Fang Liang; John Wityak; Alan Koder; Leo Vargas; Russell D. Romeo; Nico Mitro; Puiying A. Mak; H. Martin Seidel; Jennifer A. Haslam; Donald Chow; Tove Tuntland; Tracy A. Spalding; Ansgar Brock; Michelle N. Bradley; Antonio Castrillo; Peter Tontonoz; Enrique Sáez

doi:10.1021/jm070453f

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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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Molteni et al. (2007) studied this question.

synapsesocial.com/papers/6a70597275498292b709c670 https://doi.org/10.1021/jm070453f

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N-Acylthiadiazolines, a New Class of Liver X Receptor Agonists with Selectivity for LXRβ

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N-Acylthiadiazolines, a New Class of Liver X Receptor Agonists with Selectivity for LXRβ

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