• Title of article

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

  • Author/Authors

    Farid Bakir، نويسنده , , Sunil Kher، نويسنده , , Madhavi Pannala، نويسنده , , Norma Wilson، نويسنده , , Trang Nguyen، نويسنده , , Ila Sircar، نويسنده , , Kei Takedomi، نويسنده , , Chiaki Fukushima، نويسنده , , James Zapf، نويسنده , , Kui Xu، نويسنده , , Shao-Hui Zhang، نويسنده , , Juping Liu، نويسنده , , Lisa Morera، نويسنده , , Lisa Schneider، نويسنده , , Naoki Sakurai، نويسنده , , Rick Jack، نويسنده , , Jie-Fei Cheng، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2007
  • Pages
    7
  • From page
    3473
  • To page
    3479
  • 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.
  • Keywords
    Liver X receptor , Virtual screening , High-throughput gene profiling , LXR agonist
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2007
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    798257

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=798257