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通过氨基酸和肽键的修饰来进行肽模拟。

Peptidomimetics via modifications of amino acids and peptide bonds.

机构信息

Department of Chemistry, Faculty of Science, Anadolu University, 26470, Eskişehir, Turkey.

出版信息

Chem Soc Rev. 2014 May 21;43(10):3575-94. doi: 10.1039/c3cs60384a. Epub 2014 Mar 13.

Abstract

Peptidomimetics represent an important field in chemistry, pharmacology and material science as they circumvent the limitations of traditional peptides used in therapy. Self-structural organizations such as turns, helices, sheets and loops can be accessed by chemical modifications of amino acids or peptides. In-depth structural and conformational analysis and structure-activity relationships (SAR) offer a way to establish peptidomimetic libraries. Herein, we review recent developments in peptidomimetics that are formed via heteroatom replacement within the native amino acid backbone. Each sub-section describes structural features, utility and preparative methods.

摘要

肽模拟物在化学、药理学和材料科学领域具有重要意义,因为它们规避了传统治疗肽的局限性。通过对氨基酸或肽的化学修饰,可以获得自身结构组织,如转角、螺旋、片层和环。深入的结构和构象分析以及结构-活性关系(SAR)为建立肽模拟物文库提供了一种方法。本文综述了通过天然氨基酸主链中的杂原子取代形成的肽模拟物的最新进展。每个小节都描述了结构特征、用途和制备方法。

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