2. Academic Validation
  3. Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

  • Bioorg Med Chem Lett. 2007 Jun 15;17(12):3473-9. doi: 10.1016/j.bmcl.2007.03.076.
Farid Bakir 1,  Sunil Kher,  Madhavi Pannala,  Norma Wilson,  Trang Nguyen,  Ila Sircar,  Kei Takedomi,  Chiaki Fukushima,  James Zapf,  Kui Xu,  Shao-Hui Zhang,  Juping Liu,  Lisa Morera,  Lisa Schneider,  Naoki Sakurai,  Rick Jack,  Jie-Fei Cheng
Affiliations

Affiliation

  • 1 Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.
PMID: 17416521 DOI: 10.1016/j.bmcl.2007.03.076
Abstract

A structurally novel liver X receptor (LXR) agonist (1) was identified from internal compound collection utilizing the combination of structure-based virtual screening and high-throughput gene profiling. Compound 1 increased ABCA1 gene expression by eightfold and SREBP1c by threefold in differentiated THP-1 macrophage cell lines. Confirmation of its agonistic activity against LXR was obtained in the co-factor recruitment and reporter transactivation assays. Structure-activity relationship studies on compound 1 are described.

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