Bismuth-Cyclized Cell-Penetrating Peptides

被引：0

作者：

Ritchey, Jeremy L. ^{[1
]}

Filippi, Lindsi ^{[1
]}

Ballard, Davis ^{[1
]}

Pei, Dehua ^{[1
]}

机构：

[1] Ohio State Univ, Dept Chem & Biochem, Columbus, OH 43210 USA

来源：

MOLECULAR PHARMACEUTICS | 2024年 / 21卷 / 10期

基金：

美国国家卫生研究院;

关键词：

bismuth; cell-penetratingpeptides; drug delivery; endosomal escape; peptide cyclization; ARGININE-RICH PEPTIDES; INTRACELLULAR DELIVERY; CYTOSOLIC DELIVERY; ENDOSOMAL ESCAPE; PROTEIN; INHIBITOR; DISCOVERY; LEADS;

D O I：

10.1021/acs.molpharmaceut.4c00688

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Intracellular delivery of biological cargos, which would yield new research tools and novel therapeutics, remains an active area of research. A convenient and potentially general approach involves the conjugation of a cell-penetrating peptide to a cargo of interest. However, linear CPPs lack sufficient cytosolic entry efficiency and metabolic stability, while previous backbone cyclized CPPs have several drawbacks including the necessity for chemical synthesis and posttranslational conjugation to peptide/protein cargos and epimerization during cyclization. We report here a new class of bismuth cyclized CPPs with excellent cytosolic entry efficiencies, proteolytic stability, and potential compatibility with genetic encoding and recombinant production.

引用

页码：5255 / 5260

页数：6

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