共查询到19条相似文献,搜索用时 62 毫秒
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利用亲和选择筛选法从组合化学库中筛选新药 总被引:1,自引:0,他引:1
组合化学方法可以产生大量的新化合物供新药筛选,但传统的逐一筛选法不能满足如此数量庞大的化合物,因此,针对混合物进行筛选显得非常重要,亲和选择筛选法利用药物作用的靶蛋白与潜在药物之间的亲和活性,使目标化合物与大量无亲和活性的化合物分离,然后只对有亲和活性的化合物进行结构鉴定,从而快速地从大量混合物中找到目标化合物,本文着重讨论了亲和选择筛选的的几种形,相应技术和在组合化学库筛选中的应用,亲和选择筛选大体分为两种方式:一种是将靶蛋白固定在支持物上,有亲和活力的化合物被保留,大量非亲和化合物被洗掉,另一种是在溶液中靶蛋白与混合物库孵育,然后利用受体配基复合物与不结合的游离化合性质的判别进行区分,亲和选择筛选法也适合于化合物的种类和含量都未知的天然提取物的筛选。 相似文献
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化学多样性空间探索与组合药物设计 总被引:3,自引:0,他引:3
本文综述组合化学的最新进展, 内容涵盖组合化学的基本概念、原理、技术, 在药物发现中的应用, 以及组合化学和其他科学技术分枝的关系。最后, 提出了组合化学工程中亟须研究的一些项目, 介绍了开展这些研究所必需的条件, 并给出了解决方案。 相似文献
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Yao Zhu-Jun 《合成化学》2004,12(Z1)
Annonaceous acetogenins, isolated from the Annonaceae plants, have been attracting worldwide attention in recent years due to their biological activities, especially as growth inhibitors of certain tumor ceils [ 1 ]. They have been shown to function by blocking complex I in mitochondria [2] as well as ubiquinone-linked NADPH oxidase in the cells of specific tumor cell lines, including some multidrug-resistant ones [3]. These features make these acetogenins excellent leads for the new antitumor agents. In our previous work, the compounds 1a to 1d (Figure 1), which relies on structure simplification while maintaining all essential functionalities of the acetogenins, was in vitro tested against several human solid tumor cell lines and showed interesting cell selectivity [4]. All four analogues show remarkable activity against the HCT-8 and HT-29 cell lines, while compound 1c was found the best [4bi. In order to further investigate the effects of key structural features, a convergent parallel fragments assembly strategy was developed [4e]. In addition, the biological relevancies of typical annonaceous acetogenin mimetics were also studied [4f]. 相似文献
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几天来,通过代表们的发言与讨论,交流了各国在化学教育方面一些好的经验和优秀研究成果,讨论了引起当前存在问题的各种因素(涉及政治、经济以及社会等诸方面),探讨了教育改革的途径,提出了一些建议和设想。通过相互学习,共同切磋,增进了各国间的相互了解,因此,这次会议是一次成功的会议,也是在中国首次举办的一次重要国际化学教育研讨会。我相信,本届会议将为下届在陕西师范大学召开的西安会议的成功奠定基础。 相似文献
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作为传感器中最重要的研究方向之一,分子印迹传感器在近十年的发展中取得了巨大进展。分子印迹聚合物膜在转换器表面的固定化方法有涂膜法、原位引发聚合法和电化学聚合法等,其中电聚合法因具有制备简单快速、膜厚可控、膜与电极附着紧密、重现性好等优点而成为极具潜力的制备方法。该文评述了基于电化学聚合技术的分子印迹传感器的主要研究进展,对聚合膜制备过程中单体的选择和模板的去除进行了讨论,对电聚合制备的印迹传感器在传感领域的分析应用进行了总结,并在此基础上对其未来发展进行了展望。 相似文献
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Dr. Yuichi Onda Dr. Gabriele Bassi Abdullah Elsayed Franziska Ulrich Sebastian Oehler Louise Plais Dr. Jörg Scheuermann Prof. Dr. Dario Neri 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(24):7160-7167
The synthesis and characterization of a novel DNA-encoded library of macrocyclic peptide derivatives are described; the macrocycles are based on three sets of proteinogenic and non-proteinogenic amino acid building blocks and featuring the use of copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) reaction for ring closure. The library (termed YO-DEL) which contains 1 254 838 compounds, was encoded with DNA in single-stranded format and was screened against target proteins of interest using affinity capture procedures and photocrosslinking. YO-DEL selections yielded specific binders against serum albumins, carbonic anhydrases and NKp46, a marker of activated Natural Killer cells. 相似文献
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本文主要综述有机化学在建立核酸的顺序测定法和自动顺序仪,在破译遗传密码,在建立核酸片段的化学合成方法,固相合成法及DNA合成仪的设计,在合成许多有生物活力的核酸分子,在发展并完善遗传工程以及新近发现酶RNA(Ribozyme)等方面的卓越贡献。最后简要地展望有机化学将对生物学发展作出进一步贡献的几个方面。 相似文献
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My Research History on the Chemical Standpoint—From Molecular Structure to Surface Science 下载免费PDF全文
Yoshitada Murata 《Chemical record (New York, N.Y.)》2015,15(3):557-594
The structure of molecules using gas electron diffraction (GED) was my graduate study. However, I was making a new apparatus for precise measurements by GED and formulated a scheme for the least‐squares analysis for a smooth continuous curve of scattering intensity. My research was completely shifted to the solid surface after moving to Gakushuin University, where I briefly studied the liquid structure of CCl4 molecules, and I then moved to the Institute for Solid State Physics, the University of Tokyo. My studies of surface science were focused on the electronic properties and related phenomena, and various experimental methods were developed. The plasmon dispersions elucidated the initial oxidation of aluminum and one‐dimensional metal on Si(001)2 × 1–K. Irreversible phase transition was discovered on MgO(001) using the LEED Kikuchi pattern. The electronic structure of the dislocation was observed on MgO(001) by the electron time‐of‐flight method. The phase transition on Si(001) and the rotational epitaxy in a K monoatomic layer on Cu(001) were found. Next, I changed to studies of the dynamical phenomena on the surface, where very low energy reactive ion scattering on metal surfaces and laser‐induced desorption caused by electronic transition of NO and CO molecules from metal surfaces were observed, and the hydrogen atom location at the surface and interface was measured with a high depth resolution using a resonance nuclear reaction of 1H + 15N2+ at 6.385 MeV. Finally, I moved to the University of Electro‐Communications and studied thin single‐crystal oxide layers on transition metals, in which the band‐gap narrowing was found, and then a Pt monoatomic layer was prepared on the α‐Al2O3 film. 相似文献