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1.
Ni—WC复合电极的结晶结构及其电化学性能的研究   总被引:2,自引:0,他引:2  
本文在优选的工艺条件下制备了Ni-WC复合电极。其SEM观察和XRD测试结果表明:复合电极中的Ni是以比Ni电极的Ni更微小的晶粒存在。复合电沉积过程中,导电性的WC微粒的存在,对基质金属Ni的电沉积方式产生了影响,使基质金属Ni几乎无择优取向性。采用循环伏安法对其电化学性能进行研究,实验结果表明:Ni-WC复合电极在碱性水溶液析氢反应中与H质子之间的吸附作用及吸附量高于Ni电极,对硝基苯的电还原反应具有比Ni电极更良好的催化活性。  相似文献
2.
新型酪氨酸激酶小分子抑制的三维药效团研究   总被引:2,自引:0,他引:2       下载免费PDF全文
通过CATALYST软件包得到了两类HER2抑制的三维药效团模型。尽管亚苄基丙二腈化合物和3-取代吲哚啉-2-酮系列化合物具有完全不同的骨架结构,但得到的药效团却具有共同的特性,这表明当这两类抑制剂和受体发生相互作用时,采用了相似的结合模式。共同的药效团模型包括一个氢键受体,一个氢键给体,一个脂肪类疏水团以及一个芳香类疏水团。根据药效团模型,我们还进行了三维构效关系的研究,结果表明得到的药效团模型具有很好的预测能力(线性回归系数R≈0.96)。药效团模型对于研究酪氨酸激酶小分子抑制剂的结构与活性关系,以及评估和预测此类未知化合物活性具人重要的意义。  相似文献
3.
HER2 (human epidermal growth factor receptor 2, erbB2, or neu) is overexpressed by a large number of tumor types and has been identified as an important target for cancer therapy. F5 is a single-chain human antibody fragment that recognizes HER2 receptor and is covalently conjugated to PEGylated lipid to form F5 conjugate (F5CG) in the product HER2 targeted STEALTH immunoliposome doxorubicin. Here we described the method development of a competitive enzyme-linked immunosorbent assay (ELISA) for the determination of total concentration of F5 conjugate in plasma samples. The method involved the biotinylation of F5CG, detergent treatment of plasma sample to solubilize F5CG into monomeric form, and competitive ELISA for solubilized F5CG competitively binding to anti-F5CG antibody with biotinylated F5CG for the determination of total F5CG in plasma. The detection range of this method was from 0.2 ng/mL to 125 ng/mL for F5CG in plasma. The lower limit of quantification (LLOQ) was 0.2 ng/mL. This method was established and used for the measurement of F5CG concentration to provide information about F5CG circulation after the administration of immunoliposome in preclinical studies.   相似文献
4.
非晶态Ni-S-Mn三元合金电极析氢行为   总被引:1,自引:0,他引:1       下载免费PDF全文
非晶态Ni-S-Mn三元合金电极析氢行为;电极;析氢电催化活性;水电解;非晶态合金  相似文献
5.
Introduction Gastriccancerisoneofthemostcommonlyen counteredmalignantdiseasesworldwide,especiallyin AsiaandAfrica[1].Thecombinationofoperation,chemotherapyandradiotherapyisusedfortreatinggas triccarcinoma.However,the5yearsurvivalrateof patientsofgastricca…  相似文献
6.
Summary We have carried out up to 8.0 ns molecular dynamics simulation on the ATP-bound complexes of EGFR and HER-2 (homology model) receptor kinase domains to explore the possible consequences of amino acid residue changes in or close to the ATP site that might provide insights for selectivity of these kinases towards ATP site inhibitors. The simulation results show the formation of a channel under Thr766 following the movement of the side chain of Gln767 away from the hinge in EGFR. In HER-2, a similar movement of Gln799 occurs, but a simultaneous movement of Arg784 towards the hinge region occurs that tends to close the channel. The movement of Arg784 in HER-2 appears to result from the absence of an anchoring residue like Asp746 in EGFR, which has been changed to Gly778 in HER-2. In EGFR, this Arg784 is held away from the hinge region by interaction with Asp746, thereby leaving the channel open. This might be an important contributory factor to differences in selectivity of the ligands between the two kinases, probably more so than the conservative change of Cys751 of EGFR to serine in HER-2 at the ATP site.  相似文献
7.
Aberrant expression of the epidermal growth factor receptor Her2 has been implicated in various malignancies including breast cancer. Monoclonal antibodies and an antibody–drug conjugate targeting Her2 have found wide clinical application. Herein, we aimed at developing Her2-specifc ligands based on peptides that have a 100-fold smaller molecular weight than antibodies. Such peptides could potentially offer advantages in the development of ligand–drug conjugates, such as ease of synthesis and conjugation, higher molecule-per-mass ratios, and better tumor penetration. Panning of large bicyclic peptide phage display libraries against Her2 yielded a range of Her2-specific ligands having different formats and binding motifs. Strong sequence similarities among several of the isolated peptides indicated that they interact with Her2 in a specific manner. The best bicyclic peptide obtained after affinity maturation bound Her2 with a KD of 304 nM. The diverse peptide ligands may offer valuable starting points for the development of high-affinity Her2 binders with potential application for tumor imaging and therapy.  相似文献
8.
以取代4-[(4-硝基苯氧基)亚甲基]哌啶为原料,经还原、取代、suzuki和加成4步反应合成了6个新型的喹唑啉衍生物(5a ~ 5f),其结构经1H NMR和ESI-MS表征.用MTT法考察了5a ~ 5f对人脐静脉内皮细胞(HUVEC),人肺癌细胞(A-549),乳腺癌细胞(MCF-7)和人早幼粒白血病细胞(HL-60)的体外活性抑制活性.结果表明:环丙基[4-[[4-[[6-[5-{[(2-甲磺酰基乙基)氨基]甲基}呋喃-2-基]喹唑啉-4-基]氨基]苯氧基]甲基]哌啶-1-基]甲基酮(5b)抑制活性最好,其IC50分别为0.55 μg·mL-1,0.18 μg·mL-1,0.27 μg·mL-1和5.24 μg·mL-1,优于阳性对照药拉帕替尼.  相似文献
9.
Fluorescent nanoparticles (FNPs) with unique optical properties may be useful as biosensors in living cancer cell imaging and cancer targeting. A novel kind of polymer fluorescent nanoparticles (PFNPs) was synthesized and its application for ovarian cancer imaging with fluorescence microscopy imaging technology was presented in this study. The PFNPs were synthesized with precipitation polymerization by using methacrylic acid (MAA) as monomer, trimethylolpropane trimethacrylate (Trim) as cross-linker, azobisisobutyronitrile (AIBN) as radical initiator and butyl rhodamine B (BTRB) as fluorescent dye. And the fluorescent dye was embedded into the three-dimensional network of the polymer when the polymer was produced. With this method the PFNPs can be prepared easily. And then the PFNPs were successfully modified with anti-Her-2 monoclonal antibody. The fluorescence probe based on anti-Her-2 monoclonal antibody conjugated PFNPs has been used to detect ovarian cancer cells with fluorescence microscopy imaging technology. The experimental results demonstrate that the anti-Her-2 monoclonal antibody conjugated PFNPs can effectively recognize ovarian cancer cells and exhibit good sensitivity and exceptional photostability, which would provide a novel way for the diagnosis and curative effect observation of ovarian cancer cells.  相似文献
10.
The presence of human epidermal growth factor type 2 (HER2) on 20-30% of human breast cancer is a prognostic indicator of more rapid disease progression and a therapeutic indicator for anti-HER2 monoclonal antibodies. Because the literature has demonstrated some discordance between primary and metastatic tumors in the same patient for expression of the HER2 marker, we set out to develop an imaging agent that could be used to assess the marker concentration in vivo in an individual patient. The pharmaceutical company Affibody® AB has optimized the specificity of Affibody® molecules for HER2. Two Affibody® molecules, a 7 kDa and an 8 kDa protein, were designed with a single carboxy terminal cysteine in order to provide a specific location for the purposes of labeling for various types of imaging. We have prepared [18F]FBEM utilizing a coupling reaction between [18F]fluorobenzoic acid and aminoethylmaleimide. We then optimized the conjugation of this radiolabeled maleimide to the free sulfhydryl of cysteine by incubating at pH 7.4 in phosphate buffered saline containing 0.1% sodium ascorbate. An overall uncorrected yield of radiolabeled Affibody® molecule of approximately 10% from [18F]fluoride was achieved in a 2 h synthesis. These conjugated Affibody® molecules were obtained with a specific activity of 2.51 ± 0.92 MBq/μg. Characterization of the product by HPLC-MS supported the conjugation of [18F]FBEM with the Affibody® molecule. The radiolabeled Affibody® molecule retained its binding specificity as demonstrated by successful imaging of xenografts expressing HER2.  相似文献
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