| 基于四氢喹啉酸骈环戊烯骨架的蛋白酪氨酸磷酸酶1B抑制剂的设计、合成及构效关系 |
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| 引用本文： | 柴茜,沈强,马兰萍,王昕,孟韬,李静雅,李佳,沈竞康.基于四氢喹啉酸骈环戊烯骨架的蛋白酪氨酸磷酸酶1B抑制剂的设计、合成及构效关系[J].高等学校化学学报,2011,32(2):306-315. |
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| 作者姓名： | 柴茜 沈强 马兰萍 王昕 孟韬 李静雅 李佳 沈竞康 |
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| 作者单位： | 中国科学院上海药物研究所新药研究国家重点实验室;中国科学院国家新药筛选中心; |
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| 基金项目： | 国家“八六三”计划项目(批准号:2006AA02Z315); 上海市科学技术委员会基金(批准号:08QH14005和08DZ2291300)资助 |
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| 摘 要： | 基于肿瘤、糖尿病等重大疾病的有限目标,选择蛋白酪氨酸磷酸酶(PTPs)家族这一生物体系中有代表性的PTP家族成员PTP1B,SHP-1,SHP-2,LAR,CDC25B及PRL-3进行研究.通过综合高通量筛选获得的"苗头"化合物结构信息,分析得到四氢喹啉骈环戊烯骨架.初步的构效关系研究表明,四氢喹啉酸骈环戊烯母核结构可...
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| 关 键 词： | 蛋白酪氨酸磷酸酶 高通量筛选 四氢喹啉酸骈环戊烯 抑制剂 |
| 收稿时间： | 2010-05-04 |
Discovery and Structure-activity Relationships of Tetrahydro-3H-cyciopenta[c]quinolines Scaffold-based Potential PTP1B Inhibitors |
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| CHAI Qian,SHEN Qiang,MA Lan-Ping,WANG Xin,MENG Tao,LI Jing-Ya,LI Jia,SHEN Jing-Kang.Discovery and Structure-activity Relationships of Tetrahydro-3H-cyciopenta[c]quinolines Scaffold-based Potential PTP1B Inhibitors[J].Chemical Research In Chinese Universities,2011,32(2):306-315. |
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| Authors: | CHAI Qian SHEN Qiang MA Lan-Ping WANG Xin MENG Tao LI Jing-Ya LI Jia SHEN Jing-Kang |
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| Institution: | CHAI Qian1,SHEN Qiang2,MA Lan-Ping1,WANG Xin1,MENG Tao1,LI Jing-Ya2,LI Jia2,SHEN Jing-Kang1(1.State Key Laboratory of Drug Research,2.The National Center for Drug Screening,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China) |
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| Abstract: | The protein tyrosine phosphatases(PTPs) constitute a family of closely related key regulatory enzymes that dephosphorylate phosphotyrosine residues in their protein substrates.Malfunctions in PTP activity are linked to various diseases,ranging from cancer to neurological disorders and diabetes.As part of a project aimed at identifying small molecular inhibitors based on PTPs family,focusing on diabetes mellitus,tumorigenesis,and infection,we performed the high-throughput screening(HTS) of a library of 48000... |
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| Keywords: | Protein tyrosine phosphatase High-throughput screening Tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid Inhibitor |
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