共查询到14条相似文献,搜索用时 62 毫秒
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从组合化学肽库中筛选亲和配基 总被引:2,自引:0,他引:2
在亲和色谱研究中 ,建立适合于某种分离对象的亲和色谱体系的关键是寻找适合的亲和配基 .小肽亲和配基具有性质稳定、合成简单、价格低及生物相容性好等特点[1] ,但这类配基也存在着亲和力弱或选择性低的缺点 .因此 ,如何寻找小肽配基以及如何提高小肽配基的亲和力和选择性的问题引起了人们的关注与重视 [1~ 3 ] .组合化学法是一种快速制备大量相关或同类化合物的革新性的方法 [4 ] ,组合肽库包括噬菌体展示肽库和合成肽库 ,这两类肽库均可用于小肽配基的筛选与优化 [1,5] .组合化学法尽管有效 ,但以小肽为目的物进行筛选时 ,往往因肽 -肽… 相似文献
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亲和色谱法筛选中药中血管紧张素转化酶抑制剂 总被引:2,自引:0,他引:2
以壳聚糖微球为载体、戊二醛(glutaraldehyde,GA)为交联剂对血管紧张素转化酶(Angiotensin converting enzyme,ACE)进行固定化.用固化的ACE作为亲和介质,利用血管紧张素转化酶抑制剂(Angiotensin convertingenzym einhibitor,ACEI)与ACE之间的亲和作用,结合高效液相色谱对亲和前后的体系进行检测,比较两者各组分色谱峰的差异,以此实现快速筛选复杂体系中的ACE抑制剂.应用赖诺普利(Lisinopril)、九肽抑制剂、依那普利(Enalapril)、培哚普利(Perindopril)、卡托普利(Captopril)等已上市的ACEI对方法进行验证,反映方法具有高度选择性.将方法应用于中药地龙及山楂筛选,发现共有5个组分与ACE有亲和作用,并且都能抑制ACE酶活性,它们对酶活性抑制的IC50值在0.45~4.62μg/mL范围.通过对亲和方法重现性考察,6次测定的相对标准偏差小于1%,说明方法可靠.提出的亲和色谱.色谱指纹差异法非常适合于从中药及天然产物等复杂混合物库中快速筛选靶点活性物质. 相似文献
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组合化学——合成化学领域的一次革命 总被引:5,自引:0,他引:5
组合化学是近十几年逐渐发展成熟起来的一个学科,它从根本上改变了化学家、生物学家以及相关学科研究人员的思维和研究方式,对科学的发展产生了革命性的影响。组合化学从创立起就与工业应用紧密联系在一起,它带动了包括新药发明和新材料研制在内的一系列高新科技产业的发展。下面简述了组合化学的起源与发展、研究方法及其对相关学科的影响和技术前景。 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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Autocrine‐Based Selection of Drugs That Target Ion Channels from Combinatorial Venom Peptide Libraries 下载免费PDF全文
Dr. Hongkai Zhang Dr. Mingjuan Du Dr. Jia Xie Xiao Liu Jingying Sun Dr. Wei Wang Xiu Xin Prof. Lourival D. Possani Dr. Kyungmoo Yea Prof. Richard A. Lerner 《Angewandte Chemie (International ed. in English)》2016,55(32):9306-9310
Animal venoms represent a rich source of pharmacologically active peptides that interact with ion channels. However, a challenge to discovering drugs remains because of the slow pace at which venom peptides are discovered and refined. An efficient autocrine‐based high‐throughput selection system was developed to discover and refine venom peptides that target ion channels. The utility of this system was demonstrated by the discovery of novel Kv1.3 channel blockers from a natural venom peptide library that was formatted for autocrine‐based selection. We also engineered a Kv1.3 blocker peptide (ShK) derived from sea anemone to generate a subtype‐selective Kv1.3 blocker with a long half‐life in vivo. 相似文献
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Affinity capillary electrophoresis is a new procedure for receptor-ligand binding studies. Since its introduction in the early 1990s, this method has proved valuable in chiral separation of racemates, the measurement of binding constants, the estimation of kinetic rate constants, the determination of stoichiometries, the investigation of electrostatic interactions, the estimation of effective charges and molecular weights of biomolecules, the characterization of enzymatic catalysis, and, most recently, combinatorial library screening in solutions. This technique demands small amounts of samples, involves no radiolabeled materials or chemically immobilized ligands, and does not require changes in spectroscopic characteristics upon binding. This paper reviews the most recent applications of affinity capillary electrophoresis in binding measurement and combinatorial library screening. 相似文献
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Selection of DNA‐Encoded Small Molecule Libraries Against Unmodified and Non‐Immobilized Protein Targets 下载免费PDF全文
Peng Zhao Zitian Chen Yizhou Li Dawei Sun Yuan Gao Prof. Yanyi Huang Prof. Xiaoyu Li 《Angewandte Chemie (International ed. in English)》2014,53(38):10056-10059
The selection of DNA‐encoded libraries against biological targets has become an important discovery method in chemical biology and drug discovery, but the requirement of modified and immobilized targets remains a significant disadvantage. With a terminal protection strategy and ligand‐induced photo‐crosslinking, we show that iterated selections of DNA‐encoded libraries can be realized with unmodified and non‐immobilized protein targets. 相似文献
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Cover Picture: Autocrine‐Based Selection of Drugs That Target Ion Channels from Combinatorial Venom Peptide Libraries (Angew. Chem. Int. Ed. 32/2016) 下载免费PDF全文
Dr. Hongkai Zhang Dr. Mingjuan Du Dr. Jia Xie Xiao Liu Jingying Sun Dr. Wei Wang Xiu Xin Prof. Lourival D. Possani Dr. Kyungmoo Yea Prof. Richard A. Lerner 《Angewandte Chemie (International ed. in English)》2016,55(32):9099-9099
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Dr. Chiara Platella Dr. Ettore Napolitano Dr. Claudia Riccardi Prof. Domenica Musumeci Prof. Daniela Montesarchio 《ChemistryOpen》2022,11(5):e202200090
DNA G-quadruplexes (G4s) are key structures for the development of targeted anticancer therapies. In this context, ligands selectively interacting with G4s can represent valuable anticancer drugs. Aiming at speeding up the identification of G4-targeting synthetic or natural compounds, we developed an affinity chromatography-based assay, named G-quadruplex on Oligo Affinity Support (G4-OAS), by synthesizing G4-forming sequences on commercially available polystyrene OAS. Then, due to unspecific binding of several hydrophobic ligands on nude OAS, we moved to Controlled Pore Glass (CPG). We thus conceived an ad hoc functionalized, universal support on which both the on-support elongation and deprotection of the G4-forming oligonucleotides can be performed, along with the successive affinity chromatography-based assay, renamed as G-quadruplex on Controlled Pore Glass (G4-CPG) assay. Here we describe these assays and their applications to the screening of several libraries of chemically different putative G4 ligands. Finally, ongoing studies and outlook of our G4-CPG assay are reported. 相似文献
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Cover Picture: Selection of DNA‐Encoded Small Molecule Libraries Against Unmodified and Non‐Immobilized Protein Targets (Angew. Chem. Int. Ed. 38/2014) 下载免费PDF全文
Peng Zhao Zitian Chen Yizhou Li Dawei Sun Yuan Gao Prof. Yanyi Huang Prof. Xiaoyu Li 《Angewandte Chemie (International ed. in English)》2014,53(38):9963-9963