Separation of α-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRα-selective …

K Motoshima, T Noguchi-Yachide, K Sugita…

Index: Motoshima, Kazunori; Noguchi-Yachide, Tomomi; Sugita, Kazuyuki; Hashimoto, Yuichi; Ishikawa, Minoru Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 14 p. 5001 - 5014

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Citation Number: 43

Abstract

Liver X receptor (LXR) α/β dual agonists are candidate medicaments for the treatment of metabolic syndrome, because their biological actions include increasing cholesterol efflux mediated by LXRβ. However, their clinical application is currently limited by their enhancing effect on triglyceride (TG) synthesis mediated by LXRα. Combination of an LXRα-selective antagonist with an LXRα/β dual agonist may overcome this disadvantage. In the present ...