Nanostapled Peptide Empowered Tumor Targeting and Programmed Release of a Therapeutic Peptide for Colorectal Cancer Therapy.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 42304966.
- Also identified by DOI 10.1021/acs.nanolett.6c01445.
- No licence information is recorded for this record.
- Because redistribution is not established, this page shows the abstract only. Follow the links below for the full text.
Abstract
Stapled peptides exhibit superior proteolytic stability and cell permeability, relative to linear peptides. However, non-specific tissue distribution precipitates dose-limiting toxicities, constraining the therapeutic implementation. Here, we designed a self-assembling nanostapled peptide (NSP) comprising hydrophilic mPEG<sub>1000</sub> groups surrounding a hydrophobic core made up of a therapeutic stapled peptide. <i>In vivo</i>, the nanostructure protected the peptide from non-target tissues, thereby improving bioavailability. Specifically, under the acidic and MMP-9-rich conditions of the tumor microenvironment, the therapeutic peptide could be released through programmed disassembly to penetrate the colorectal cancer cells and activate a downstream apoptotic pathway. Collectively, this study establishes NSP as a promising platform for the precise and effective treatment of colorectal cancers.