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静远嘲风封面设计作品-亚洲化学

已有 1873 次阅读 2015-3-6 12:58 |个人分类:发表作品|系统分类:论文交流

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期刊:
Chemistry – An Asian Journal

Volume 10, Issue 3, page 768, March 2015 

原文标题:
Rational Design of Selenadiazole Derivatives to Antagonize Hyperglycemia-Induced Drug Resistance in Cancer Cells

原文作者:
Yuedan Liu, Yi Luo, Dr. Xiaoling Li, Dr. Wenjie Zheng and Dr. Tianfeng Chen

原文摘要:
Hyperglycemia is an important factor for chemoresistance of hepatocellular carcinoma patients with diabetes to therapeutics. In the present study, a series of selenadiazole derivatives have been rationally designed, synthesized, and found be able to antagonize drug resistance in HepG2 cells to doxorubicin (DOX) under simulated diabetes conditions. Hyperglycemia could promote the cell proliferation through upregulation of ERK and AKT phosphorylation. However, the synthetic selenadiazole derivatives effectively potentiated the cellular uptake of DOX and enhanced the antiproliferative activity of DOX on HepG2 cells by induction of apoptosis, via regulation of ROS-mediated AMPK activation, inhibition of mTORC1, and an increase in DNA damage. The selenadiazole derivatives that possess an increased lipophilicity could enhance the cellular uptake and anticancer efficacy of DOX. Taken together, this study provides a rational design strategy of selenadiazole derivatives to overcome hyperglycemia-induced drug resistance.t al. report on the rational design of selenadiazole derivatives that could antagonize the drug resistance of HepG2 hepatocellular carcinoma cells to anticancer drugs under simulated diabetes conditions, through overproduction of reactive oxygen species (ROS), activation of adenosine monophosphate-activated kinase (AMPK), and inhibition of mTOR Complex1 (mTORC1). This study may provide an effective strategy to design selenadiazole derivatives with the potency to overcome hyperglycemia-induced drug resistance.

原文链接:
http://onlinelibrary.wiley.com/doi/10.1002/asia.201403409/abstract




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