Synthesis and biological evaluation of an epidermal growth factor receptor-targeted peptide-conjugated phthalocyanine-based photosensitiser

摘要: A peptide-conjugated zinc(II) phthalocyanine containing the epidermal growth factor receptor-targeted heptapeptide QRHKPRE has been prepared. The conjugate labelled as ZnPc-QRH* can selectively bind to cell membrane of HT29 human colorectal adenocarcinoma cells in 10 min followed by internalisation upon prolonged incubation via receptor-mediated endocytosis, leading localisation lysosomes eventually. By manipulating time, subcellular be varied and cell-death pathways induced irradiation also altered. It found that photosensitisation initiated at would trigger death mainly through necrosis apoptosis respectively. Intravenous administration into tumour-bearing nude mice resulted higher accumulation tumour than most major organs. selective binding this demonstrated comparing results with those analogue a scrambled peptide sequence (EPRQRHK). overall indicate is promising EGFR-targeted photosensitiser for photodynamic therapy.