Efficacy of inverso isomer of CendR peptide on tumor tissue penetration.

ABSTRACT: The dense extracellular matrix and high interstitial fluid pressure of tumor tissues prevent the ability of anti-tumor agents to penetrate deep into the tumor parenchyma for treatment effects. C-end rule (CendR) peptides can enhance the permeability of tumor blood vessels and tumor tissues via binding to neuropilin-1 (NRP-1), thus aiding in drug delivery. In this study, we selected one of the CendR peptides (sequence RGERPPR) as the parent l-peptide and substituted d-amino acids for the l-amino acids to synthesize its inverso peptide _D(RGERPPR). We investigated the NRP-1 binding activity and tumor-penetrating ability of _D(RGERPPR). We found that the binding affinity of _D(RGERPPR) with NRP-1 and the cellular uptake was significantly higher than that o

SUBMITTER: Wang R 

PROVIDER: S-EPMC6146380 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature