2. Academic Validation
  3. Discovery and optimization of a novel series of liver X receptor-alpha agonists

Discovery and optimization of a novel series of liver X receptor-alpha agonists

  • Bioorg Med Chem Lett. 2006 Mar 15;16(6):1638-42. doi: 10.1016/j.bmcl.2005.12.015.
Leping Li 1,  Jiwen Liu,  Liusheng Zhu,  Serena Cutler,  Hirohiko Hasegawa,  Bei Shan,  Julio C Medina
Affiliations

Affiliation

  • 1 Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. leping1@amgen.com
PMID: 16386417 DOI: 10.1016/j.bmcl.2005.12.015
Abstract

A novel series of hexafluorocarbinols were discovered as potent activators of the liver X receptor-alpha using a fluorescence polarization assay. Structure-activity relationship study led to the identification of compounds that are more potent agonists than the endogenous ligand, 24(S), 25-epoxycholesterol, with similar efficacy. Several compounds, including T0901317, were shown to have desirable pharmacokinetic profiles suitable for in vivo studies.

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