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• W4320481405 endingPage "1590" @default.
• W4320481405 startingPage "1577" @default.
• W4320481405 abstract "To investigate the structure-cellular penetration relationship of guanidinium-rich transporters (GRTs), we previously designed PGua4, a five-amino acid peptoid containing a conformationally restricted pattern of eight guanidines, which showed high cell-penetrating abilities and low cell toxicity. Herein, we characterized the cellular uptake selectivity, internalization pathway, and intracellular distribution of PGua4, as well as its capacity to deliver cargo. PGua4 exhibits higher penetration efficiency in HeLa cells than in six other cell lines (A549, Caco-2, fibroblast, HEK293, Mia-PaCa2, and MCF7) and is mainly internalized by clathrin-mediated endocytosis and macropinocytosis. Confocal microscopy showed that it remained trapped in endosomes at low concentrations but induced pH-dependent endosomal membrane destabilization at concentrations ≥10 μM, allowing its diffusion into the cytoplasm. Importantly, PGua4 significantly enhanced macropinocytosis and the cellular uptake and cytosolic delivery of large IgGs following noncovalent complexation. Therefore, in addition to its peptoid nature conferring high resistance to proteolysis, PGua4 presents characteristics of a promising tool for IgG delivery and therapeutic applications." @default.
• W4320481405 created "2023-02-14" @default.
• W4320481405 creator A5000738142 @default.
• W4320481405 creator A5010324058 @default.
• W4320481405 creator A5010870371 @default.
• W4320481405 creator A5020281637 @default.
• W4320481405 creator A5028087747 @default.
• W4320481405 creator A5041509652 @default.
• W4320481405 creator A5041729989 @default.
• W4320481405 date "2023-02-13" @default.
• W4320481405 modified "2023-10-06" @default.
• W4320481405 title "Characterization of PGua₄, a Guanidinium-Rich Peptoid that Delivers IgGs to the Cytosol via Macropinocytosis" @default.
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