Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists

F Bakir, S Kher, M Pannala, N Wilson, T Nguyen…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3473 - 3479

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Citation Number: 13

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 ...