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肽模拟物——代谢稳定且具有生物活性的分子中金属结合基序的无限资源库。

Peptidomimetics - An infinite reservoir of metal binding motifs in metabolically stable and biologically active molecules.

机构信息

Faculty of Chemistry, University of Wroclaw, Joliot - Curie 14, Wroclaw 50-383, Poland.

Faculty of Chemistry, University of Wroclaw, Joliot - Curie 14, Wroclaw 50-383, Poland.

出版信息

J Inorg Biochem. 2021 Apr;217:111386. doi: 10.1016/j.jinorgbio.2021.111386. Epub 2021 Feb 10.

Abstract

The involvement of metal ions in interactions with therapeutic peptides is inevitable. They are one of the factors able to fine-tune the biological properties of antimicrobial peptides, a promising group of drugs with one large drawback - a problematic metabolic stability. Appropriately chosen, proteolytically stable peptidomimetics seem to be a reasonable solution of the problem, and the use of D-, β-, γ-amino acids, unnatural amino acids, azapeptides, peptoids, cyclopeptides and dehydropeptides is an infinite reservoir of metal binding motifs in metabolically stable, well-designed, biologically active molecules. Below, their specific structural features, metal-chelating abilities and antimicrobial potential are discussed.

摘要

金属离子在与治疗性肽相互作用中的参与是不可避免的。它们是能够微调抗菌肽生物学特性的因素之一,抗菌肽是一组很有前途的药物,但存在一个大问题 - 代谢稳定性差。选择合适的、蛋白水解稳定的肽类似物似乎是解决这个问题的合理方法,使用 D-、β-、γ-氨基酸、非天然氨基酸、氮杂肽、肽缩醛、环肽和去氢肽为代谢稳定、精心设计、具有生物活性的分子提供了无限的金属结合基序。下面讨论了它们的特定结构特征、金属螯合能力和抗菌潜力。

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