Significance
Accumulating documents indicate tumor cell-mediated vasculogenic mimicry (VM) is positively correlated with poor prognosis, occurrence of distant metastasis and low survival rate in cancer patients, suggesting VM is a potential therapeutic target for cancer treatment. Thus, effective anti-angiogenic strategies should simultaneously inhibit VM as well as endothelium-dependent vessels (EDV). Integrin αvβ3 is a crucial inducer involved in the formation of both EDV and VM. In this study, we engineered αvβ3 integrin-targeting peptide cRGD functionalized nanoparticles (cRGD-NPs) by self-assembly using heparin conjugated with cRGD and folate. The prepared cRGD-NPs represent a promising anti-angiogenic medicine in that they are able to inhibit endothelial sprouting angiogenesis and tumor cell-mediated VM. This work may provide useful information with which to construct effective anti-angiogenic nanomedicines.
Statement of significance
Accumulating documents indicate tumor cell-mediated vasculogenic mimicry (VM) is positively correlated with poor prognosis, occurrence of distant metastasis and low survival rate in cancer patients, suggesting VM is a potential therapeutic target for cancer treatment. Thus, effective anti-angiogenic strategies should simultaneously inhibit VM as well as endothelium-dependent vessels (EDV). Integrin αvβ3 is a crucial inducer involved in the formation of both EDV and VM. In this study, we engineered αvβ3 integrin-targeting peptide cRGD functionalized nanoparticles (cRGD-NPs) by self-assembly using heparin conjugated with cRGD and folate. The prepared cRGD-NPs represent a promising anti-angiogenic medicine in that they are able to inhibit endothelial sprouting angiogenesis and tumor cell-mediated VM. This work may provide useful information with which to construct effective anti-angiogenic nanomedicines.