All-in-one peptide with sequential pH gradient sensing capabilities for the targeted delivery and deep penetration of nanomicelles against breast cancer.

ABSTRACT: Antitumor nanomedicines are usually decorated with ligands to achieve multiple functions, such as targeting delivery, tissue penetration and enhanced cellular uptake. However, a single ligand with multiple functions is generally preferred for use in practice. Herein, a versatile peptide, (HE)₁₀G₅R₆GDK (HE-RK), was engineered by integrating several motifs into a single sequence, including a masking segment (HE), a flexible linker (G₅), and a tumor-penetrating head (RK) which comprised a cell-penetrating peptide (R₆) and a C-end Rule peptide (RGDK). The RK moiety in HE-RK was sequentially activated following the gradual charge reversal of HE to facilitate the accumulation of its cargos in deep tumor tissue and the cytosol of cancer cells

SUBMITTER: Chen Q 

PROVIDER: S-EPMC12329104 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature