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以DNA拓扑异构酶Ⅱ为靶点的抗癌药物 被引量:4
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作者 蒙凌华 张永炜 丁健 《中国新药杂志》 CAS CSCD 北大核心 2002年第9期675-683,共9页
DNA拓扑异构酶Ⅱ (TopoisomeraseⅡ ,TOPOⅡ )是一种真核生物生存所必需的泛酶 ,在几乎所有DNA代谢过程中发挥重要作用。TOPOⅡ使一条完整的DNA双链穿过一个移过性的双链断口 ,从而导致DNA解结或解旋。因为TOPOⅡ具有重要的生理功能 ,... DNA拓扑异构酶Ⅱ (TopoisomeraseⅡ ,TOPOⅡ )是一种真核生物生存所必需的泛酶 ,在几乎所有DNA代谢过程中发挥重要作用。TOPOⅡ使一条完整的DNA双链穿过一个移过性的双链断口 ,从而导致DNA解结或解旋。因为TOPOⅡ具有重要的生理功能 ,它已成为抗癌药物的重要作用靶点。以TOPOⅡ为靶点的药物按作用方式可分为 2类 :一类通过稳定TOPOⅡ介导的可切割复合物而杀死肿瘤细胞 ,称为TOPOⅡ毒剂 (TOPOⅡpoison) ;另一类通过抑制TOPOⅡ的催化活性而达到抑制肿瘤的作用 ,称为TOPOⅡ催化抑制剂 (TOPOⅡinhibi tor)。近年来 ,对TOPOⅡ催化机制和药物作用方式的研究取得了很大进展 ,这些发现有助于进一步了解TOPOⅡ的生理功能 ,进而研究出更有效的治疗方案和新的抗癌药。本文介绍了以TOPOⅡ为靶点的抗癌药物的作用机制及其发展现状。 展开更多
关键词 抗癌药物 拓扑异构酯Ⅱ 肿瘤 生物学特性
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DNA复制过程中的拓扑异构作用
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作者 柴培春 《生物学通报》 北大核心 1996年第8期22-22,共1页
DNA复制过程中的拓扑异构作用柴培春(山东省枣庄市台儿庄区职业中专277400)DNA在复制时两条链要解开,此时必然产生张力,早期认为这种张力的消除是靠两条链的高度旋转来解决的。甚至现在有些遗传学方面的书还是这样认为... DNA复制过程中的拓扑异构作用柴培春(山东省枣庄市台儿庄区职业中专277400)DNA在复制时两条链要解开,此时必然产生张力,早期认为这种张力的消除是靠两条链的高度旋转来解决的。甚至现在有些遗传学方面的书还是这样认为。但对于很细长的核酸链来说,处于细... 展开更多
关键词 DNA 复制 拓扑异构
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国产三维CAD系统数据转换接口技术研究 被引量:2
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作者 王启富 高东 +1 位作者 黄运保 刘俊 《机械科学与技术》 CSCD 北大核心 2005年第12期1478-1481,共4页
CAD系统之间的数据交换是三维CAD系统的重要组成部分,也是难点问题。本文重点对国产三维CAD系统在与其它典型商用CAD系统进行数据转换过程中出现的拓扑异构、几何间隙等问题进行了研究,并给出了相应的解决方法。这些方法已被成功地应用... CAD系统之间的数据交换是三维CAD系统的重要组成部分,也是难点问题。本文重点对国产三维CAD系统在与其它典型商用CAD系统进行数据转换过程中出现的拓扑异构、几何间隙等问题进行了研究,并给出了相应的解决方法。这些方法已被成功地应用于三维数据转换接口的开发中,并取得了较好的实用效果。 展开更多
关键词 3D-CAD 数据交换 拓扑异构 几何间隙
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胃癌组织中多药耐药性的研究 被引量:9
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作者 刘连新 綦书抑 +1 位作者 姜洪池 朱安龙 《实用癌症杂志》 2000年第2期148-150,共3页
目的 研究胃癌组织中DNA拓扑异构酶 (topoisomerase ,TopoⅡ ) ,谷胱甘肽S 转移酶 ( glutathioneS transferases ,GST π)和P 糖蛋白 (P glycoprotein ,P gp)表达的意义。 方法 应用免疫组织化学S P法对 98例胃癌进行检测。结果 在 9... 目的 研究胃癌组织中DNA拓扑异构酶 (topoisomerase ,TopoⅡ ) ,谷胱甘肽S 转移酶 ( glutathioneS transferases ,GST π)和P 糖蛋白 (P glycoprotein ,P gp)表达的意义。 方法 应用免疫组织化学S P法对 98例胃癌进行检测。结果 在 98例胃癌中 ,74例 ( 75 .5 %)GST π表达阳性 ,5 6例 ( 5 7.1%)P 糖蛋白表达阳性 ,TopoⅡ计数 (TopoⅡLI)为 11.1%~ 3 8.2 %。三者均与胃癌的分化程度有关 (P <0 .0 5 ) ,而与患者的年龄、性别、肿瘤的大小、部位、浸润程度和淋巴结转移情况无关。结论 联合检测TopoⅡ ,GST π和P gp对胃癌的治疗有一定的指导意义。 展开更多
关键词 胃肿瘤 DN-1拓扑异构 P-糖蛋白 GST
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慎用氟喹诺酮类抗生素 被引量:2
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作者 沈叙庄 杨永弘 《中国处方药》 2003年第3期50-53,共4页
氟喹诺酮类抗生素是一类作用于抑制细菌DNA促旋酶与DNA拓扑异构酶IV的药物。 近年来上市的许多新型氟喹诺酮类抗生素,比如莫西沙星、加替沙星以及正在开发研究中的西他沙星、吉米沙星等药物,它们能比较平衡地作用于DNA旋转酶与DNA拓扑... 氟喹诺酮类抗生素是一类作用于抑制细菌DNA促旋酶与DNA拓扑异构酶IV的药物。 近年来上市的许多新型氟喹诺酮类抗生素,比如莫西沙星、加替沙星以及正在开发研究中的西他沙星、吉米沙星等药物,它们能比较平衡地作用于DNA旋转酶与DNA拓扑异构酶IV两个位点,抗菌性能优于主要作用DNA促旋酶的早期喹诺酮类药物。 展开更多
关键词 氟喹诺酮类抗生素 莫西沙星 加替沙星 DNA旋转酶 DNA拓扑异构
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光缆/互联网/大数据/WWW/IoT的创新过程中美高能合作旋进-旋出第4次工业革命的人文科学、技术经济Ⅱ
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作者 沈经 《仪器仪表标准化与计量》 2016年第4期1-8,共8页
2016中国跟进2010日本第四次工业革命、2011德国工业4.0、2012美国互联网工业而成最大互联网商国。本文分析发明"互联网+"三部曲:全球光缆网、互联互通的TCP/IP Internet、教科文技工商交流内容的超文本标准WWW及其搜索引擎Go... 2016中国跟进2010日本第四次工业革命、2011德国工业4.0、2012美国互联网工业而成最大互联网商国。本文分析发明"互联网+"三部曲:全球光缆网、互联互通的TCP/IP Internet、教科文技工商交流内容的超文本标准WWW及其搜索引擎Google的发明创新过程。 展开更多
关键词 ICT革命 大科学旋进-旋出新产业 中美异构拓扑管理网络的网关 TCP/IP 管理科学CPN
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光缆/互联网/大数据/WWW/IoT的创新过程中美高能合作旋进-旋出第4次工业革命的人文科学、技术经济Ⅰ
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作者 沈经 《仪器仪表标准化与计量》 2016年第3期16-22,共7页
介绍互联网ISO-OSI数据链路层和网络层的发明与引进过程。1979-1989邓小平与Carter签订《中美科技文化合作协定》中的合作建北京正负电子对撞机BEPC-北京谱仪BES期间,Stanford发明以太网、工作站、路由器,继发明复印机的Xerox,创SUN、Ci... 介绍互联网ISO-OSI数据链路层和网络层的发明与引进过程。1979-1989邓小平与Carter签订《中美科技文化合作协定》中的合作建北京正负电子对撞机BEPC-北京谱仪BES期间,Stanford发明以太网、工作站、路由器,继发明复印机的Xerox,创SUN、Cisco。SLAC的创新是:用互联网前身BITnet+HEPnet改革工程管理,以小胜大赢CERN巨无霸!1992-1994高能所许榕生最先从SLAC"Spin in"互联网。1994航天第二研究院706所沈崧率队请教许榕生开始"Spin off"工业应用。1995中科院张树新创民用瀛海威。 展开更多
关键词 ICT革命 大科学旋进-旋出新产业 中美异构拓扑管理网络的网关 TCP/IP管理科学CPN
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Adeno-associated virus mediated endostatin gene therapy in combination with topoisomerase inhibitor effectively controls liver tumor in mouse model 被引量:6
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作者 SungYiHong MyunHeeLee +5 位作者 WooJinHyung SungHoonNoh SeungHoChoi Kyung Sup Kim HyunCheolJung JaeKyungRoh 《World Journal of Gastroenterology》 SCIE CAS CSCD 2004年第8期1191-1197,共7页
AIM:rAAV mediated endostatin gene therapy has been examined as a new method for treating cancer.However, a sustained and high protein delivery is required to achieve the desired therapeutic effects.We evaluated the im... AIM:rAAV mediated endostatin gene therapy has been examined as a new method for treating cancer.However, a sustained and high protein delivery is required to achieve the desired therapeutic effects.We evaluated the impact of topoisomerase inhibitors in rAAV delivered endostatin gene therapy in a liver tumor model. METHODS:rAAV containing endostatin expression cassettes were transduced into hepatoma cell lines.To test whether the topoisomerase inhibitor pretreatment increased the expression of endostatin,Western blotting and ELISA were performed.The biologic activity of endostatin was confirmed by endothelial cell proliferation and tube formation assays. The anti-tumor effects of the rAAV-endostatin vector combined with a topoisomerase inhibitor,etoposide,were evaluated in a mouse liver tumor model. RESULTS:Topoisomerase inhibitors,including camptothecin and etoposide,were found to increase the endostatin exPression level in vitro.The over-expressed endostatin, as a result of pretreatment with a topoisomerase inhibitor, was also biologically active.In animal experiments,the combined therapy of topoisomerase inhibitor,etoposide with the rAAV-endostatin vector had the best tumor- suppressive effect and tumor foci were barely observed in livers of the treated mice.Pretreatment with an etoposide increased the level of endostatin in the liver and serum of rAAV-endostatin treated mice.Finally,the mice treated With rAAV-endostatin in combination with etoposide showed the longest survival among the experimental models. CONCLUSION:rAAV delivered endostatin gene therapy in combination with a topoisomerase inhibitor pretreatment is an effective modality for anticancer gene therapy. 展开更多
关键词 ADENOVIRIDAE Animals Antineoplastic Agents Antineoplastic Agents Phytogenic CAMPTOTHECIN Carcinoma Hepatocellular Cell Line Tumor Combined Modality Therapy DNA Topoisomerases inhibitors Drug Synergism ENDOSTATINS Endothelium Vascular Enzyme Inhibitors ETOPOSIDE Gene Expression Gene Therapy Humans Liver Neoplasms Mice Research Support Non-U.S. Gov't SARCOMA Survival Rate Umbilical Veins
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Cellular processing determinants for the activation of damage signals in response to topoisomerase I-linked DNA breakage
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作者 Ting-Hsiang Huang Hsiang-Chin Chen Shang-Min Chou Yu-Chen Yang Jia-Rong Fan Tsai-Kun Li 《Cell Research》 SCIE CAS CSCD 2010年第9期1060-1075,共16页
Recent studies have suggested an involvement of processing pathways for the initiation of cellular responses induced by topoisomerase-targeting drugs. Here, we showed that cellular exposure to camptothecin (CPT) ind... Recent studies have suggested an involvement of processing pathways for the initiation of cellular responses induced by topoisomerase-targeting drugs. Here, we showed that cellular exposure to camptothecin (CPT) induced formation of topoisomerase I cleavable complex (TOPlcc), degradation of TOP1 and activation of DNA damage responses (DDR). Transcription and proteasome-dependent proteolysis, but not replication, were involved in CPTo indneed TOPl degradation, while none of above three processing activities affected TOPlcc formation. Replication- and transcription-initiated proeessing (RIP and TIP) of TOPlee were identified as two independent pathways, which contribute distinctly to various CPT-activated DDR. Specifically, in cycling cells, RIP-processed TOPlec triggered the CPT-induced RPA pbosphorylation. At higher CPT dosages, the TIP pathway is required for other DDR activation, including ATM, p53 and Chkl/2 phosphorylation. The TIP pathway was further demonstrated to be S-phase independent by using three nonreplicating cell models. Furthermore, the effect of proteasome inhibitors mimicked that of transcription inhibition on the CPT-induced activation of DDR, suggesting the involvement of proteasome in the TIP pathway. Interestingly, the TIP pathway was important for TOPlcc-activated, but not ionization radiationactivated ATM, p53 and Chk2 phosphorylation. We have also found that pharmacological interferences of TIP and RIP pathways distinctively modulated the CPT-induced cell killing with treatments at low and high dosages, respec- tively. Together, our results support that both RIP and TIP pathways of TOPlcc are required for the activation of CPT-induced DDR and cytotoxicity. 展开更多
关键词 cleavable complex PROCESSING DOWNREGULATION protein-linked DNA break DNA damage responses
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S-1 induced secondary acute erythroid leukemia with a chromosome inv(12)(p13;q13)
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作者 Kensuke Matsumoto Akira Kitanaka +5 位作者 Makiko Uemura Fusako Waki Tetsuya Fukumoto Hiroaki Ohnishi Yoshitsugu Kubota Toshihiko Ishida 《World Journal of Gastroenterology》 SCIE CAS CSCD 2011年第41期4632-4634,共3页
Adjuvant chemotherapy by S-1 following gastrectomy is considered standard treatment in Japan.Analysis of follow-up data have proved the effi cacy of S-1 admin-istration,and that hematological adverse events were relat... Adjuvant chemotherapy by S-1 following gastrectomy is considered standard treatment in Japan.Analysis of follow-up data have proved the effi cacy of S-1 admin-istration,and that hematological adverse events were relatively rare.Pyrimidine anti-metabolites,including S-1,have shown relatively lower risks for secondary hematological malignancies in comparison to alkylat-ing agents and topoisomerase-Ⅱ inhibitors.We here report a case of therapy-related leukemia after S-1 administration.A patient who had received S-1as the sole adjuvant chemotherapy was diagnosed with acute erythroid leukemia.To the best of our knowledge,our patient represents the fi rst report of S-1 induced acute leukemia. 展开更多
关键词 S-1 Secondary leukemia Acute erythroidLeukemia Gastric cancer
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Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening
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作者 张虹 潘远江 《Journal of Zhejiang University Science》 EI CSCD 2004年第8期900-905,共6页
A method of screening assay is demonstrated. The approach is based on the affinity of antitumor candidates for topoisomerases. In this method, antitumor candidates are fished out using topoisomerases as targets. Tradi... A method of screening assay is demonstrated. The approach is based on the affinity of antitumor candidates for topoisomerases. In this method, antitumor candidates are fished out using topoisomerases as targets. Traditional analysis of complex compounds typically encounters signal suppression due to the relatively low concentrations, but enzyme-affinity screening for the active compounds can effectively concentrate the desired analysts into a small volume of high concen-tration. Active compounds are separated from non-affinity compounds by ultrafiltration. The molecules-enzymes complexes that are retained on the filter are subsequently separated by acidification to obtain the topoisomerases-affinity compounds for analysis on High Performance Liquid Chromatography coupled with electrospray ionization mass spectrometric detec-tion (ESI-MS). This enzyme-affinity based screening assay provides a highly specific and efficient method that can directly screen, identify, and acquire drug candidates thus improving the accuracy and speed of high-throughput screening activities. 展开更多
关键词 AFFINITY High-throughput screening LC-MS TOPOISOMERASE ULTRAFILTRATION
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Nutritional Composition and Topoisomerase Inhibitor Activity of Ethnomedicinal Marine Mollusk Nerita albicilla
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作者 Linawati Hardjito Dani Sjafardan Royani Joko Santoso 《Journal of Food Science and Engineering》 2012年第10期550-556,共7页
DNA topoisomerases (topo) I and II are molecular targets of several potent anticancer agents. Thus, inhibitors of these enzymes are potential candidates for anticancer development. Traditionally, Nerita albicilla ha... DNA topoisomerases (topo) I and II are molecular targets of several potent anticancer agents. Thus, inhibitors of these enzymes are potential candidates for anticancer development. Traditionally, Nerita albicilla had been used in Kei Island, Southern Maluku, Indonesia to treat liver disease including cancer. The paper reports on the chemical composition ofNerita albicilla and its topo I inhibitor ofhexane, ethyl acetate and methanol extracts. Topoisomerase-I inhibitor activity was determined using the method reported by TopoGEN. The proximate analysis described that Nerita albicilla dried powder contained 12.45% ± 0.05% moisture; 9.17% ± 0.03% ash; 62.05% ± 0.10% protein; 5.58% ± 0.08% fat; 6.60% ± 0.02% crude fiber and 4.15% ± 0.24% carbohydrate (by difference). Furthermore, the protein consisted of 11 essential amino acids and six non-essential amino acids. It contained significant amount of branched-chain amino acids (BCAA) valine, leucine, isoleucine (a total of 187.8 mg g-1 protein) and lower content of aromatic amino acids phenylalanine, tyrosine and histidine (a total of 111.26 mg .g-1 protein). The protein score was 92.2. The yield of hexane, ethyl acetate and methanol extracts ofNerita albicilla were 2.05% ± 0.05%, 1.56% ± 0.06% and 6.99% ± 0.14%, respectively. All extracts showed topoisomerase-I inhibitor activities. Minimum inhibitory concentration (MIC) of methanol extract was 2.50 ug mL-1. Chemical screening of the extracts showed that they contained steroidal and alkaloid compounds. The investigation revealed that Nerita albicilla contains active compounds that could be potential for nutraceutical or pharmaceutical development. 展开更多
关键词 Nerita albicilla nutritional composition topoisomerase-I inhibitor.
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Analysis on Refinery System as a Complex Task-resource Network 被引量:4
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作者 刘苏昱 荣冈 《Chinese Journal of Chemical Engineering》 SCIE EI CAS CSCD 2013年第3期253-262,共10页
Refinery system, a typical example of process systems, is presented as complex network in this paper. The topology of this system is described by task-resource network and modeled as directed and weighted graph, in wh... Refinery system, a typical example of process systems, is presented as complex network in this paper. The topology of this system is described by task-resource network and modeled as directed and weighted graph, in which nodes represent various tasks and edges denote the resources exchanged among tasks. Using the properties of node degree distribution, strength distribution and other weighted quantities, we demonstrate the heterogeneity of the network and point out the relation between structural characters of vertices and the functionality of correspond- ing tasks. The above phenomena indicate that the design requirements and principles of production process contrib- ute to the heterogeneous features of the network. Besides, betweenness centrality of nodes can be used as an impor- tance indicator to provide additional information for decision making. The correlations between structure and weighted properties are investigated to further address the influence brought by production schemes in system con- nectivity patterns. Cascading failures model is employed to analyze the robustness of the network when targeted at- tack happens. Two capacity assignment strategies are compared in order to improve the robustness of the network at certain cost. The refinery system displays more reliable behavior when the protecting strategy considers heteroge- neous properties. This phenomenon further implies the structure-activity relationship of the refinery system and provides insightful suggestions for process system design. The results also indicate that robustness analysis is a _promising applicat!on of methodologies from complex networks to process system engineering.. 展开更多
关键词 zomplex network refinery system structure-activity relationship HETEROGENEITY robusmess
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LRIG1在胶质瘤细胞系U251细胞中的作用 被引量:2
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作者 刘宝辉 陈谦学 +7 位作者 李明昌 郭振涛 朱晓楠 冀保卫 董慧敏 吴立权 田道锋 易伟 《中华神经医学杂志》 CAS CSCD 北大核心 2013年第10期980-985,共6页
目的探讨多亮氨酸重复区免疫球蛋白样蛋白I(LRIG1)在胶质瘤细胞系U251细胞中的作用及引起的相关基因变化。方法以PEGFP-LRIG1质粒转染体外常规培养的U251细胞,同时设PEGFP-N1组和空白组作为对照,RT-PCR检测3组细胞LRIG1、GDNF、拓... 目的探讨多亮氨酸重复区免疫球蛋白样蛋白I(LRIG1)在胶质瘤细胞系U251细胞中的作用及引起的相关基因变化。方法以PEGFP-LRIG1质粒转染体外常规培养的U251细胞,同时设PEGFP-N1组和空白组作为对照,RT-PCR检测3组细胞LRIG1、GDNF、拓扑异构酶Ⅱ(TOPOII)基因表达的变化。Westernblotting检测细胞LRIGl蛋白的表达;绘制PEGFP-N1和PEGFP-LRIGl组细胞1-5d的生长曲线并计算替莫唑胺对2组细胞的抑制率。应用siGDNF和siLRIGl敲低U251细胞中GDNF和LRIG1的表达.同时设单纯siGDNF、siLRIGl组和空白组作为对照,比较细胞增殖率的变化。结果3组细胞LRIG1基因和蛋白、TOPOII和GDNF基因表达不同,差异有统计学意义(P〈0.05);与PEGFP-N1组和空白组比较,PEGFP-LRIG1组细胞LRIG1基因和蛋白的表达较高,TOPOll和GDNF基因表达较低,差异均有统计学意义(P〈0.05)。细胞生长1~5d时,PEGFP—LRIGl组细胞计数低于PEGFP-N1组,差异有统计学意义俨〈0.05)。加入替莫唑胺培养后,PEGFP—LRIGl组细胞抑制率高于PEGFP-N1组,差异有统计学意义(P〈0.05)。Westernblotting结果显示应用siGDNF和siLRIG1敲低LRIGJ和GDNF成功。siLRIGl组细胞抑制率高于对照组,siLRIGl+siGDNF组胞抑制率低于siLRIGl组,差异均有统计学意义(P〈0.05)。结论LRIG1可以通过调节GDNF的表达来调节U251细胞的生长:LRIG1可以抑制GDNF、TOPOU的表达,提高胶质瘤细胞对替莫唑胺的化疗敏感性。 展开更多
关键词 多亮氨酸重复区免疫球蛋白样蛋白1 胶质细胞源性神经生长因子 拓扑异构 酶Ⅱ U251细胞 细胞增殖
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耐药基因蛋白和Ki67在原发性肝癌中的表达及其在预后中的价值 被引量:7
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作者 郭飞宇 杨军 +3 位作者 熊书名 高森 朱茂群 李建平 《中华肝脏外科手术学电子杂志》 CAS 2018年第1期77-81,共5页
目的探讨P-糖蛋白(Pgp)、胎盘型谷胱甘肽-S-转移酶(GST-π)、拓扑异构酶Ⅱ(TopoⅡ)和胸苷酸合酶(TS)4种耐药基因蛋白及Ki67在原发性肝癌(肝癌)中的表达及其在预后中的价值。方法标本来源于2008年3月至2016年12月在南通大学第三附属医院... 目的探讨P-糖蛋白(Pgp)、胎盘型谷胱甘肽-S-转移酶(GST-π)、拓扑异构酶Ⅱ(TopoⅡ)和胸苷酸合酶(TS)4种耐药基因蛋白及Ki67在原发性肝癌(肝癌)中的表达及其在预后中的价值。方法标本来源于2008年3月至2016年12月在南通大学第三附属医院接受诊治的41例肝癌患者。患者均签署知情同意书,符合医学伦理学规定。其中男26例,女15例;平均年龄(56±10)岁。采用免疫组化法检测肝癌组织中Pgp、GST-π、TopoⅡ、TS和Ki67的表达水平。相关性分析采用Spearman相关分析,生存率分析采用Kaplan-Meier法和Log-rank检验,患者的预后影响因素采用Cox比例风险回归模型分析。结果 Pgp、GST-π、TopoⅡ、TS和Ki67在肝癌组织中存在阳性表达,阳性率分别为73%(30/41)、7%(3/41)、61%(25/41)、39%(16/41)和51%(21/41)。TS表达与Pgp、TopoⅡ表达呈正相关(r_s=0.484,0.333;P<0.05)。生存分析结果显示TS和Ki67阳性患者和阴性患者生存情况差异有统计学意义(χ~2=4.695,5.784;P<0.05)。Cox多因素回归分析显示TS和Ki67为影响患者总体预后的独立危险因素(HR=3.007,17.108;P<0.05)。结论 Pgp、GST-π、TopoⅡ、TS在肝癌中均有表达,且TS和Pgp、TopoⅡ的表达呈正相关,TS和Ki67是影响患者预后的独立危险因素。 展开更多
关键词 多药耐药相关蛋白质类 p-糖蛋白 谷胱甘肽S-转移酶pi DNA拓扑异构 酶类 胸苷酸合酶 肝肿瘤 预后 危险因素
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Synthesis of podophyllotoxin derivative GL331 and identification of it binding site on topoisomerase IIα with molecular modeling 被引量:1
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作者 胡炽文 刘鹰翔 《Journal of Chinese Pharmaceutical Sciences》 CAS 2010年第1期34-37,共4页
A facile one-pot procedure has been developed for the synthesis of GL331 in 26% overall yield.In addition,molecular modeling study was carried out to predict the binding site of GL331 with human topoisomerase IIα.The... A facile one-pot procedure has been developed for the synthesis of GL331 in 26% overall yield.In addition,molecular modeling study was carried out to predict the binding site of GL331 with human topoisomerase IIα.The result showed that GL331 exhibited high affinity for the ATPase domain of human topoisomerase IIα and suggested that GL331 probably acts as a competitor of ATP for binding with the human topoisomerase IIα. 展开更多
关键词 Synthesis GL331 Topoisomerase IIα Molecular docking
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Synthesis and biological evaluation of indeno[1, 2-b]indole derivatives as dual topoisomerase Ⅰ & Ⅱ inhibitors: novel multidrug resistant reversal anticancer agents
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作者 Dongbo Lu Yu Chen +4 位作者 Shan Liu Chao Guo Xia Li Zhongjun Li Xiangbao Meng 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2019年第11期786-801,共16页
A single compound able to inhibit both TopoⅠandⅡmay present the advantage of improving anti-proliferative activity,with reduced toxic side effects,with respect to the combination of two inhibitors.We designed and sy... A single compound able to inhibit both TopoⅠandⅡmay present the advantage of improving anti-proliferative activity,with reduced toxic side effects,with respect to the combination of two inhibitors.We designed and synthesized 28 compounds of indeno[1,2-b]indole derivatives as a new class of TopoⅠandⅡinhibitor and successfully identified compound 2-3 j,which showed the most potent cell growth inhibition with IC50=0.74μM against HCT-116 cell line.Compound 2-3 j was also evaluated as a potent topoisomeraseⅠandⅡinhibitor and can induce apoptosis in human colon cancer cells.2-3 j showed potency against a small panel of drug sensitive and multidrug resistant(MDR)cell lines,and it reversed the MDR of K562/A02,MCF-7/Adr,and KB/Vcr cells at 0.5μM,with reversal fold values of 3.2,10.1,and 5.8,respectively.2-3 j might inhibit the function of ABCG2 to increase intracellular drug accumulation and enhance the sensitivity of conventional chemotherapeutic agents for MDR cells.2-3 j could be a promising lead for the development of a new class of antitumor drug acting as inhibitors of TopoⅠ&Ⅱand ABCG2. 展开更多
关键词 Indeno[1 2-b]indole ANTI-CANCER TopoisomerseⅠ&Ⅱinhibitor Reverse multi-drug resistance
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Majorana zero mode in the vortex of an artificial topological superconductor
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作者 Hao-Hua Sun Jin-Feng Jia 《Science China(Physics,Mechanics & Astronomy)》 SCIE EI CAS CSCD 2017年第5期49-59,共11页
Majorana fermion (MF), an exotic particle that is identical to its own antiparticle, was recently found in solid matter as a quasiparticle excitation, the Majorana zero mode (MZM), in the vortex of an artificial t... Majorana fermion (MF), an exotic particle that is identical to its own antiparticle, was recently found in solid matter as a quasiparticle excitation, the Majorana zero mode (MZM), in the vortex of an artificial topological superconductor (TSC). This artificial TSC, first proposed by Fu and Kane in 2008, is a heterostructure made of a topological insulator BiETe3 and an s-wave superconductor NbSe2. This paper will briefly review the experimental progresses based on the Bi2Te3/NbSe2 heterostructure. All evidences are self-consistent and reveal that the MZM exists in the center of vortex. Those experimental results are also supported by theory. This finding is a milestone in the research ofMajorana fermions in solid state physics and a starting point of MZM's application in topological quantum computation. 展开更多
关键词 Majorana fermion Majorana zero mode topological superconductor HETEROSTRUCTURE VORTEX
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