|
|||||
|
|
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists |
|
| Authors: | Bakir Farid Kher Sunil Pannala Madhavi Wilson Norma Nguyen Trang Sircar Ila Takedomi Kei Fukushima Chiaki Zapf James Xu Kui Zhang Shao-Hui Liu Juping Morera Lisa Schneider Lisa Sakurai Naoki Jack Rick Cheng Jie-Fei |
| Affiliation: | Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA. |
| 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: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |