944707-85-1Relevant articles and documents
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists
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
, p. 3473 - 3479 (2008/09/19)
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.