Structure–activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6 …

…, M Nakagomi, M Makishima, M Ishikawa…

Index: Nishiyama, Yuko; Nakamura, Masahiko; Misawa, Takashi; Nakagomi, Madoka; Makishima, Makoto; Ishikawa, Minoru; Hashimoto, Yuichi Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 9 p. 2799 - 2808

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Citation Number: 8

Abstract

Abstract Retinoic acid receptor-related orphan receptors (RORs), which belong to the nuclear receptor superfamily, regulate many physiological processes, including hepatic gluconeogenesis, lipid metabolism, immune function and circadian rhythm. Since RORs resemble liver X receptors (LXRs) in the fold structure of their ligand-binding domains, we speculated that ROR-mediated transcription might be modulated by LXR ligands, in line ...

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