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      candidate compounds
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  候选化合物
     To search database and pick up candidate compounds based 3D structure of HER2/neu tyrosine kinase domain.
     根据 HER2/neu酪氨酸激酶 ATP结合区的空间结构,搜索数据库,找出候选化合物
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  “candidate compounds”译为未确定词的双语例句
     We evaluated the inhibitory effects of 43 candidate compounds on COX-1 and COX-2 using this assay system and obtained IC_(50) value of 32 compounds.
     利用该模型我们共测定了43个化合物在不同浓度下对COX-1和COX-2的抑制作用,获得了32个化合物对COX-2或COX-1的半数抑制浓度。
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     Results and Conclusion Active candidate compounds including MOPMC, 2FBMPC, MPTMBC, DMHPPP and PPVP were shown to antagonize thrombosis at the dose of 1 mg·kg -1 through activating the endothelial target for acetylcholine;
     结果 化合物MOPMC ,2FBMPC ,MPTMBC ,DMHPPP和PPVP在 1 0mg·kg- 1 可显著降低成栓率 ;
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     In vitro alternative model to assess toxicity and screen leading candidate compounds at early stage of drug development is one of the targets in discovery toxicology.
     而利用体外细胞模型在药物开发早期对先导化合物进行毒性评价和优化筛选是发现毒理学研究的发展趋势之一;
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     AIM Our investigation is to screen bioactive novel compounds using the isolated rat aortic rings and depending on the similar and distinct characteristics between the endothelial target for acetylcholine(ETA) and muscarinic receptors and to investigate the mechanisms of vasodilatory effects of candidate compounds.
     目的 利用ETA与M受体的相似性和差异性 ,设计合成吗啉环和哌嗪环类新结构化合物 ,分析其对血管舒张功能的影响。
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  相似匹配句对
     On the nonstoichiometric compounds
     浅谈非整比化合物
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     On the Compounds in GuoYu
     《国语》复音词研究
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     THEORY FOR DETERMINING CANDIDATE KEYS
     候选关键字的判定理论
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  candidate compounds
The cloned transporters can be used in mammalian expression systems for screening candidate compounds identified during drug discovery and development and in the in vivo prediction of the pharmacokinetics of therapeutic agents.
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Three candidate compounds were identified from pheromone gland extracts of female moths, using gas chromatography (GC), GC-electroantennographic detection and GC-mass spectrometric analyses, in conjunction with dimethyldisulfide derivatization.
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Fly models have turned out to be excellent system for the in vivo testing of therapeutic potentials of candidate compounds.
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The effect is not mimicked by a number of candidate compounds (including auxins, cytokinins, polyamines and vitamins).
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The present study focuses on the discovery of candidate compounds that inhibit the association between microorganisms and fibronectin.
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         Objective: To discover HER2/neu tyrosine kinase inhibitor through computer- aided drug design approach. Methods: The three- dimensional(3D) structure of HER2/neu and EGFR tyrosine kinase domain was modeled using MODERLAR software. To search database and pick up candidate compounds based 3D structure of HER2/neu tyrosine kinase domain. Inhibition of HER2/neu tyrosine kinase phosphorylation by the compounds was detected using Western blot analysis. Inhibition of cell proliferation was determ...
            目的:用计算机辅助设计法寻找 HER2/neu受体酪氨酸激酶小分子抑制剂。方法:用 MODERLAR软件模拟出 HER2/neu和 EGFR受体酪氨酸激酶的三维 (three- dimensional,3D)空间结构;根据 HER2/neu酪氨酸激酶 ATP结合区的空间结构,搜索数据库,找出候选化合物;用 Western blot方法检测化合物对 HER2/neu受体酪氨酸激酶磷酸化的影响; MTT法检测细胞增殖抑制作用。结果:比较 HER2/neu和 EGFR(靶蛋白)与胰岛素受体酪氨酸激酶、 FGFR1受体酪氨酸激酶和 Src酪氨酸激酶(模板蛋白)的氨基酸序列发现有 35%~ 41%的相同和 52%~ 55%的相似,用 MODELLER程序模拟出 HER2/neu和 EGFR激酶区域的 3D结构。根据 HER2/neu受体酪氨酸激酶结构模型, 3D数据库的搜索,获得潜在 HER2/neu酪氨酸激酶抑制剂化合物,经筛选、优化发现 ST2325对 HER2/neu磷酸化有明显的抑制作用,其 IC50值为 6.6μ mol/L,且抑制作用是可逆的,对 EGFR受体磷酸化没有抑制作用。 ST2325对 HER2/...
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         AIM: To develop a whole-cell assay based on murine peritoneal macrophages and evaluate the inhibitory effect of candidate compounds on cyclooxygenase-1 (COX-1) and COX-2. METHODS: Macrophages were stimulated with calcimycin or lipopolysaccharide (LPS) for various periods. Their abilities to convert endogenous arachidonic acid to 6-keto-PGF1α or PGE2 were examined by radioimmunoassay (RIA). RNA level of glyceraldehyde-3-phos-phate dehydrogenase (GAPDH) and COX-1/2 was detected by reverse transcri...
            目的:建立腹腔巨噬细胞模型评价化合物对环氧酶1和2的抑制作用.方法:放免法测定calcimycin、脂多糖刺激细胞将内源性花生四烯酸转化为6-keto-PGF_(1α)或PGE_2的量.GAPDH和环氧酶1/2的RNA用RT-PCR测定.结果:Rofecoxib选择性抑制脂多糖诱导的PGE_2合成,IC_(50)为(4.7±0.5)nmol/L,而抑制calcimycin诱导的6-keto-PGF_(1α)合成最大抑制率为17.3%.吲哚美辛对环氧酶1和2的IC_(50)分别为(4.7±1.1)nmol/L和(7.1±1.2)nmol/L.17个化合物中,系列Ⅱ化合物的活性与rofecoxib相当.磺酰胺基和内酰胺环的相对位置对抑制环氧酶2的活性很重要.结论:模型适用于药物设计的体外评价.3,4-二苯基-3-吡咯啉-2-酮衍生物有望成为新的环氧酶2选择性抑制剂.
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         AIM Our investigation is to screen bioactive novel compounds using the isolated rat aortic rings and depending on the similar and distinct characteristics between the endothelial target for acetylcholine(ETA) and muscarinic receptors and to investigate the mechanisms of vasodilatory effects of candidate compounds. METHODSIn isolated rat aorta precontracted with NE, the vasodilatory effects of novel structure compounds were investigated. We Compared the maximal relaxation of endothe...
            目的 利用ETA与M受体的相似性和差异性 ,设计合成吗啉环和哌嗪环类新结构化合物 ,分析其对血管舒张功能的影响。方法 采用离体大鼠胸主动脉环 ,观察化合物对血管张力的影响 ;并观察L NAME ,吲哚美辛和阿托品对血管环最大舒张率的影响。结果  81个化合物中有 57个能舒张血管 ,其中 8个最大舒张率在 50 %~ 85 % ;活性化合物按母核可分为 8类 ;DMHPPP和PPVP诱发的内皮依赖性舒血管反应可被L NAME和吲哚美辛所拮抗 ,但不被阿托品拮抗 ;DMHPPP和PPVP还能显著增强乙酰胆碱 (ACh)诱发的内皮依赖性舒血管反应的最大舒张率。结论 具有舒血管作用的活性化合物通过促进内皮细胞释放一氧化氮(NO)和前列环素 (PGI2 )共同实现舒张效应 ;并可调节血管内皮细胞乙酰胆碱靶标的功能
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