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Encoded combinatorial libraries for the construction of cyclic peptoid microarrays

机译:编码的组合文库,用于构建环状类肽微阵列

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摘要

A "one bead two compound" approach to the synthesis of encoded cyclic peptoid libraries is reported.rnDrug-like small molecules (<500 Daltons) generally do not bind well to the relatively shallow surfaces of proteins involved in protein-protein interactions. Thus, in order to develop effective therapeutic agents against these increasingly important targets, it is necessary to develop libraries of compounds able to cover a greater surface area and engage in multiple contacts with the target protein, as well as efficient methods to screen these libraries. With regard to their protein-binding properties, peptides are an attractive class of molecules, but linear peptides have many undesirable features.
机译:报道了一种“一珠两化合物”的方法来合成编码的环状拟肽文库。药物样小分子(<500道尔顿)通常不能很好地结合蛋白质-蛋白质相互作用中相对较浅的蛋白质表面。因此,为了开发针对这些日益重要的靶标的有效治疗剂,有必要开发能够覆盖更大表面积并与靶蛋白进行多次接触的化合物的文库,以及筛选这些文库的有效方法。关于它们的蛋白质结合特性,肽是一类有吸引力的分子,但是线性肽具有许多不良特性。

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  • 来源
    《Chemical Communications》 |2008年第44期|5704-5706|共3页
  • 作者

    Yong-Uk Kwon; Thomas Kodadek;

  • 作者单位

    Division of Translational Research, Departments of Internal Medicine and Molecular Biology, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA Department of Chemistry and Nano Science, Ewha Womans University, 120-750 Seoul, South Korea;

    Division of Translational Research, Departments of Internal Medicine and Molecular Biology, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA;

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