| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377618 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
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.
Graphical abstractA structurally novel LXR agonist (1) was identified utilizing the combination of virtual screening and high-throughput gene profiling. Structure–activity relationship studies on 1 are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
