Discovery and Structure–activity Relationship Studies of Indole Derivatives As Liver X Receptor (LXR) Agonists
Bioorganic & medicinal chemistry letters(2007)
摘要
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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关键词
virtual screening,high-throughput gene profiling,LXR agonist,liver X receptor
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