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 ,
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
