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Confocal laser scanning microscopy results indicated that free DOX mainly accumulated in the nuclei of both TfR overexpressed HepG2 hepatoma cells and L\u2010O2 normal liver cells expressing low level of TfR; most of the BP9a\u2010DOX conjugate displayed cytoplasmic location, and its cellular uptake by HepG2 cells was obviously reduced by TfR blockage test. Nevertheless, the cellular uptake of this conjugate by L\u2010O2 cells was much less than that of free DOX. Meanwhile, the BP9a\u2010DOX conjugate exhibited lower in vitro antiproliferative activity against HepG2 cells than free DOX, but its cytotoxic effect on L\u2010O2 cells was decreased compared with that of free DOX. These results suggest that BP9a could be applied as a potential TfR\u2010targeted peptide vector for selective drug delivery.<\/jats:p>","DOI":"10.1111\/cbdd.13613","type":"journal-article","created":{"date-parts":[[2019,8,27]],"date-time":"2019-08-27T04:08:50Z","timestamp":1566878930000},"page":"58-65","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Design, synthesis, and in vitro antitumor activity of a transferrin receptor\u2010targeted peptide\u2013doxorubicin conjugate"],"prefix":"10.1111","volume":"95","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9924-5686","authenticated-orcid":false,"given":"Songtao","family":"Li","sequence":"first","affiliation":[{"name":"Hebei Province Key Laboratory of Research and Development of Traditional Chinese Medicine Institute of Chinese Mateia Medica Chengde Medical University Chengde 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