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

ABSTRACT: 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 the cell membrane of HT29 human colorectal adenocarcinoma cells in 10 min followed by internalisation upon prolonged incubation via receptor-mediated endocytosis, leading to localisation in lysosomes eventually. By manipulating the incubation time, the subcellular localisation of the conjugate can be varied and the cell-death pathways induced upon irradiation can also be altered. It has been found that photosensitisation initiated at the cell membrane and in the lysosomes would trigger cell death mainly through necrosis and apoptosis respectively. Intravenous administration of the con

SUBMITTER: Xue EY 

PROVIDER: S-EPMC9065697 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature