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

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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 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 conjugate into HT29 tumour-bearing nude mice resulted in higher accumulation in the tumour than in most major organs. The selective binding of this conjugate to tumour has also been demonstrated by comparing the results with those of the analogue with a scrambled peptide sequence (EPRQRHK). The overall results indicate that ZnPc-QRH* is a promising EGFR-targeted photosensitiser for photodynamic therapy.
出版社接受日期21.06.2019
著者Evelyn Y. Xue, Roy C. H. Wong, Clarence T. T. Wong, Wing-Ping Fong, Dennis K. P. Ng
期刊名稱RSC Advances
出版年份2019
月份7
卷號9
期次36
出版社The Royal Society of Chemistry
頁次20652 - 20662
國際標準期刊號2046-2069
語言英式英語

上次更新時間 2020-18-10 於 02:59