Discovery of a new binding mode for a series of liver X receptor agonists.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA.

Published: April 2012

Structural modification of a series of dual LXRα/β agonists led to the identification of a new class of LXRβ partial agonists. An X-ray co-crystal structure shows that a representative member of this series, pyrrole 5, binds to LXRβ with a reversed orientation compared to 1.

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http://dx.doi.org/10.1016/j.bmcl.2012.02.028DOI Listing

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