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SR9243

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https://www.readbyqxmd.com/read/29670908/liver-x-receptor-inverse-agonist-sr9243-suppresses-nonalcoholic-steatohepatitis-intrahepatic-inflammation-and-fibrosis
#1
Peng Huang, Benson Kaluba, Xiao-Lin Jiang, Shi Chang, Xiao-Feng Tang, Lin-Feng Mao, Zhi-Peng Zhang, Fei-Zhou Huang
Abnormal metabolism of cholesterol may be a contributing factor in nonalcoholic steatohepatitis (NASH) pathogenesis. Accumulating evidence has shown that liver X receptor (LXR) is closely related to intrahepatic inflammation and fibrosis. In this study, we evaluated the effects of a novel liver-specific LXR inverse agonist, SR9243, on antifibrosis in NASH mice. A high-cholesterol diet was employed to induce NASH in BALB/c mice by either carbon tetrachloride (CCL4) administration or bile-duct ligation (BDL)...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29324503/%C3%AE-asarone-alleviated-chronic-constriction-injury-induced-neuropathic-pain-through-inhibition-of-spinal-endoplasmic-reticulum-stress-in-an-liver-x-receptor-dependent-manner
#2
Yulong Gui, Aiyuan Li, Jie Zhang, Guan Li, Xia Ruan, Qulian Guo, Wangyuan Zou
BACKGROUND: Neuropathic pain is an intractable and complex disease. Recent studies have shown a close relationship between endoplasmic reticulum (ER) stress and neuropathic pain. Here, we investigated the effect of α-asarone, an ER stress inhibitor, on chronic constriction injury (CCI)-induced neuropathic pain. METHODS: Two parts were included in this study. In part 1, rats were assigned to 7 groups: the sham group, the sham + α-asarone 20 mg/kg group, the CCI group, the CCI + vehicle group, the CCI + α-asarone 5 mg/kg group, the CCI + α-asarone 10 mg/kg group, and the CCI + α-asarone 20 mg/kg group...
January 9, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/26120082/broad-anti-tumor-activity-of-a-small-molecule-that-selectively-targets-the-warburg-effect-and-lipogenesis
#3
Colin A Flaveny, Kristine Griffett, Bahaa El-Dien M El-Gendy, Melissa Kazantzis, Monideepa Sengupta, Antonio L Amelio, Arindam Chatterjee, John Walker, Laura A Solt, Theodore M Kamenecka, Thomas P Burris
Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress. The nuclear receptor liver-X-receptor (LXR) directly regulates expression of key glycolytic and lipogenic genes. To disrupt these oncogenic metabolism pathways, we designed an LXR inverse agonist SR9243 that induces LXR-corepressor interaction. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression...
July 13, 2015: Cancer Cell
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