Liver X receptors (LXR) belong to the nuclear hormone receptor superfamily, which are ligand-inducible transcription factors regulating various genes through interactions with DNA response elements and transcription co-regulators.  Both isoforms of LXR (LXRa and LXR�) are involved in the regulation of cholesterol and lipid metabolism; LXRa and LXR� have become important targets for treatment of atherosclerosis.  The ligand binding domain of LXR� has been investigated by X-ray crystallography; and more recently, the structure of the retinoid X receptor a (RXRa)-LXR� heterodimer on DNA was solved. A number of LXR modulators have been reported.  Here we describe the discovery of a novel series of LXR� modulators starting from a phenyl sulfone fragment.

Structure-based design of novel liver X receptor modulators

248th National Meeting (2014)

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