Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2012 Apr 1;22(7):2407-10. doi: 10.1016/j.bmcl.2012.02.028. Epub 2012 Feb 20.
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.
对一系列双重 LXRα/β激动剂进行结构修饰,鉴定出了一类新型 LXRβ部分激动剂。X 射线共晶结构表明,该系列的代表性成员吡咯 5 与 LXRβ的结合方式与 1 相反。