Mitochondria-Targeting Peptoids

被引：34
作者：
Nam, Ho Yeon [1 ]
Hong, Jong-Ah [4 ]
Choi, Jieun [1 ]
Shin, Seungheon [2 ]
Cho, Steve K. [2 ,3 ]
Seo, Jiwon [1 ]
Lee, Jiyoun [4 ]
机构：
[1] Gwangju Inst Sci & Technol, Sch Phys & Chem, Dept Chem, Gwangju 61005, South Korea
[2] Gwangju Inst Sci & Technol, Sch Life Sci, Gwangju 61005, South Korea
[3] Gwangju Inst Sci & Technol, Dept Biomed Sci & Engn, Gwangju 61005, South Korea
[4] Sungshin Univ, Dept Global Med Sci, Seoul 01133, South Korea
来源：
BIOCONJUGATE CHEMISTRY | 2018年 / 29卷 / 05期
基金：
新加坡国家研究基金会;
关键词：
SOLID-PHASE SYNTHESIS; SIDE-CHAINS; CANCER-THERAPY; DELIVERY; PROBES; OLIGOMERS; PEPTIDES; THERAPEUTICS; TRANSPORTERS; DYSFUNCTION;
D O I：
10.1021/acs.bioconjchem.8b00148
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：1669 / 1676
页数：8
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