Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors

…, M Nakamura, M Nakamura, Y Matsumoto…

Index: Toyama, Hirozumi; Nakamura, Masaharu; Nakamura, Masahiko; Matsumoto, Yotaro; Nakagomi, Madoka; Hashimoto, Yuichi Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 6 p. 1948 - 1959

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Citation Number: 4

Abstract

Abstract Retinoic acid receptor (RAR)-related orphan receptors (RORs) regulate a variety of physiological processes, including hepatic gluconeogenesis, lipid metabolism, circadian rhythm and immune function. The RAR agonist: all-trans retinoic acid was reported to be an RORβ inverse agonist, but no information is available regarding ROR activity of its synthetic analogue Am580. Therefore, we screened Am580 and some related ...