Mitochondria-Targeting Peptoids,Bioconjugate Chemistry

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Mitochondria-Targeting Peptoids
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2018-03-26 00:00:00 , DOI: 10.1021/acs.bioconjchem.8b00148
Ho Yeon Nam , Jong-Ah Hong ₁ , Jieun Choi , Seungheon Shin , Steve K. Cho , Jiwon Seo , Jiyoun Lee ₁

Affiliation

Mitochondria-specific delivery methods offer a valuable tool for studying mitochondria-related diseases and provide breakthroughs in therapeutic development. Although several small-molecule and peptide-based transporters have been developed, peptoids, proteolysis-resistant peptidomimetics, are a promising alternative to current approaches. We designed a series of amphipathic peptoids and evaluated their cellular uptake and mitochondrial localization. Two peptoids with cyclohexyl residues demonstrated highly efficient cell penetration and mitochondrial localization without significant adverse effects on the cells and mitochondria. These mitochondria-targeting peptoids could facilitate the selective and robust targeted delivery of bioactive compounds, such as drugs, antioxidants, and photosensitizers, with minimal off-target effects.

中文翻译：

线粒体靶向肽

线粒体特异的递送方法为研究线粒体相关疾病提供了有价值的工具，并在治疗开发方面取得了突破。尽管已经开发了几种基于小分子和肽的转运蛋白，但类肽，耐蛋白水解的拟肽类药物是当前方法的有前途的替代方法。我们设计了一系列两亲性类肽，并评估了它们的细胞摄取和线粒体定位。具有环己基残基的两个类肽表现出高效的细胞渗透和线粒体定位，而对细胞和线粒体没有明显的不利影响。这些靶向线粒体的类肽可以促进对生物活性化合物（如药物，抗氧化剂和光敏剂）的选择性和稳固靶向递送，而产生的脱靶效应最小。

更新日期：2018-03-26

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