Efficacy of inverso isomer of CendR peptide on tumor tissue penetration

• DOI: 10.1016/j.apsb.2018.06.006
• Publication Date: 2018-06-30T07:57:13Z
• Authors: Ruifeng Wang; Qing Shen; Xue Li; Cao Xie; Weiyue Lu; Songli Wang; Jing Wang; Dongli Wang; Min Liu
• Keywords: Parenchyma; Oligopeptide

The dense extracellular matrix and high interstitial fluid pressure of tumor tissues prevent the ability anti-tumor agents to penetrate deep into parenchyma for treatment effects. C-end rule (CendR) peptides can enhance permeability blood vessels via binding neuropilin-1 (NRP-1), thus aiding in drug delivery. In this study, we selected one CendR (sequence RGERPPR) as parent l-peptide substituted d-amino acids l-amino synthesize its inverso peptide D(RGERPPR). We investigated NRP-1 activity tumor-penetrating found that affinity D(RGERPPR) with cellular uptake was significantly higher than RGERPPR. Evans Blue tests revealed exhibited improved C6, U87 A549 tumor-bearing nude mice. Using mice bearing xenograft tumors a model, rate growth group co-administered gemcitabine (Gem) lower gemcitabine-treated suppression (TSR%) 55.4%. Together, our results demonstrate is potential peptide.