The Medicinal Chemistry of Liver X Receptor (LXR) Modulators

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• 作者：Colin M. Tice ; Paul B. Noto ; Kristi Yi Fan ; Linghang Zhuang ; Deepak S. Lala ; Suresh B. Singh
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：September 11, 2014
• 年：2014
• 卷：57
• 期：17
• 页码：7182-7205
• 全文大小：868K
• ISSN：1520-4804

文摘

LXRs have been of interest as targets for the treatment of atherosclerosis for over a decade. In recent years, LXR modulators have also garnered interest for potential use in the treatment of inflammation, Alzheimer鈥檚 disease (AD), dermatological conditions, hepatic steatosis, and oncology. To date, no LXR modulator has successfully progressed beyond phase I clinical trials. In this Perspective, we summarize published medicinal chemistry efforts in the context of the available crystallographic data, druglikeness, and isoform selectivity. In addition, we discuss the challenges that need to be overcome before an LXR modulator can reach clinical use.