Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development

Parveen Kumar; Nalini Yadav; Aruna Chhikara; Madhu Chopra

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Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development

机译：组合固相合成的最近进展：技术，表征及其在药物开发中的应用

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Combinatorial chemistry has rapidly evolved from its interest in the generation of large number of compounds for the discovery of actives amongst them in random screening procedure to a powerful designed combinatorial technology for the creation and optimization of pharmaceutical lead compounds to produce drug candidates. The introduction of solid phase synthesis methods has rich impulse in this field, through automation and miniaturization. This review summarizes the present techniques of solid phase synthesis associated with combinatorial chemistry. The conventional methods for the synthesis of peptide libraries on solid support are split and mix synthesis, pre-mixed synthesis and parallel synthesis. In order to fulfil the increasing demand of synthetic peptides, several techniques have been developed,for example, pin synthesis, tea-bag synthesis, photolithography, SPOT synthesis, microchip synthesis, nanotechnology, lab-on-a-chip and bioinformatics and further their deconvolution to access the contribution of every peptide to the desired biological activity. This review also discusses about the combinatorial peptide library characterization and purity as well as their applications in drug development.

机译：组合化学从其对大量化合物的兴趣迅速发展，以便在随机筛选过程中发现活性物质，以强大为设计的组合技术，用于制作和优化药物铅化合物以产生药物候选物。通过自动化和小型化引入固体合成方法的引入具有富脉冲。该综述总结了与组合化学相关的固相合成的本技术。用于合成固体载体的肽文库的常规方法是分裂和混合合成，预混合合成和平行合成。为了满足合成肽的不断增加，已经开发了几种技术，例如引脚合成，茶袋合成，光刻，点合成，微芯片合成，纳米技术，芯片和生物信息学，并进一步去卷积以获得每种肽的贡献到所需的生物活性。该评价还讨论了组合肽库表征和纯度以及它们在药物开发中的应用。

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来源
《Current Biochemical Engineering》 |2017年第1期|共25页
作者
Parveen Kumar; Nalini Yadav; Aruna Chhikara; Madhu Chopra;
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作者单位

Department of Chemistry Dyal Singh College University of Delhi Lodhi Road Delhi 110003 India;

Dr. B. R. Ambedkar Center for Biomedical Research University of Delhi Delhi 110007 India;

Department of Chemistry Dyal Singh College University of Delhi Lodhi Road Delhi 110003 India;

Dr. B. R. Ambedkar Center for Biomedical Research University of Delhi Delhi 110007 India;

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原文格式 PDF
正文语种 eng
中图分类生物化学;生物工程学（生物技术）;
关键词
Solid phase peptide synthesis; combinatorial chemistry; deconvolution; high throughput screening; pharmaceutical;

机译：固相肽合成;组合化学;解卷积;高通量筛选;制药;

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1. Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development [J] . Parveen Kumar, Nalini Yadav, Aruna Chhikara, Current Biochemical Engineering . 2017,第1期

机译：组合固相合成的最近进展：技术，表征及其在药物开发中的应用
2. Molecularly imprinted microspheres for the anticancer drug aminoglutethimide: Synthesis, characterization, and solid-phase extraction applications in human urine samples [J] . Jia-Ping Lai, Fang Chen, Hui Sun, Journal of separation science. . 2014,第9a10期

机译：分子印迹微球用于抗癌药氨基谷氨酰胺：在人类尿液样品中的合成，表征和固相萃取应用
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机译：核磁共振方法识别结合到单个固相合成珠的非破坏性化合物的组合化学应用
4. Simultaneous multiple synthesis by the Multipin~TM method: Techniques for multiple handling, high throughput characterization and reaction optimization on solid phase [C] . Andrew m.Bray, N.Joe Maeji, Liana M.Lagniton, Chinese peptide symposium . 1998

机译：MultiPin〜TM方法同时进行多种合成：固相多处理的技术，高通量表征和反应优化
5. Synthetic strategies for solid-phase synthesis: I. Design, synthesis, and applications of handles. II. Combinatorial synthesis of small molecules. [D] . Kappel, Joseph Charles. 2003

机译：固相合成的合成策略：I.手柄的设计，合成和应用。二。小分子的组合合成。
6. Computer programs in nucleic acid synthesis: synthetic strategy development using solid-phase chemical techniques with data storage retrieval and analysis capabilities. [O] . S Lombardi, H Seidell, S Pulford, 1984

机译：核酸合成中的计算机程序：使用具有数据存储检索和分析功能的固相化学技术开发合成策略。
7. Synthesis, Characterization of Silica Gel Phases-Chemically Immobilized-4-Aminoantipyrene and Applications in the Solid Phase Extraction, Preconcentration and Potentiometric Studies [O] . Mohamad M. OSMAN, Sherif A. KHOLEIF, Nevine A. ABOU-ALMAATY, 2004

机译：合成，硅胶阶段 - 化学固定 - 4-氨基丙烯和固相萃取，前浓缩和电位研究中的应用的特征

Recent Progress in Combinatorial Solid Phase Synthesis: Techniques, Characterization and its Application in Drug Development

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