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Traditional cancer therapies prolong the life expectancy of patients but often suffer from adverse reactions. Photodynamic Therapy (PDT) has been recommended as a treatment option for lung cancer in several countries, due to its non-invasive procedures, high selectivity and weak side effects.<\/jats:p><\/jats:sec><jats:sec><jats:title>Objective:<\/jats:title><jats:p>We have designed and synthesized a biotin receptor-targeted silicon phthalocyanine (IV) (compound 1) which showed a good therapeutic effect on biotin receptor-positive tumors. Since the overexpression of Biotin Receptor (BR) is also present in human lung cancer cells (A549), we explored the therapeutic properties of compound 1 on A549 xenograft tumor models.<\/jats:p><\/jats:sec><jats:sec><jats:title>Methods:<\/jats:title><jats:p>The selectivity of compound 1 toward A549 cells was studied with a fluorescence microscope and IVIS Spectrum Imaging System. The cytotoxicity was measured using the MTT assay. In vivo anti-tumor activity was investigated on the nude mice bearing A549 xenografts.<\/jats:p><\/jats:sec><jats:sec><jats:title>Results:<\/jats:title><jats:p>In vitro assays proved that compound 1 could selectively accumulate in A549 cells via the BR-mediated internalization. In vivo imaging and distribution experiments showed that compound 1 could selectively accumulate in tumor tissues of tumor-bearing mice. After 16 days of the treatment, the volumes of tumor in the PDT group were obviously smaller than that in other groups.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion:<\/jats:title><jats:p>This study demonstrates that compound 1 is a promising photosensitizer and has broad application prospects in clinical PDT of lung cancers.<\/jats:p><\/jats:sec>","DOI":"10.2174\/1389201021666200510001627","type":"journal-article","created":{"date-parts":[[2020,5,10]],"date-time":"2020-05-10T06:10:38Z","timestamp":1589091038000},"page":"414-422","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":18,"title":["Targeted Photodynamic Therapy (PDT) of Lung Cancer with Biotinylated Silicon (IV) Phthalocyanine"],"prefix":"10.2174","volume":"22","author":[{"given":"Wenyi","family":"Dong","sequence":"first","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9588-0412","authenticated-orcid":true,"given":"Ke","family":"Li","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shijie","family":"Wang","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ling","family":"Qiu","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qingzhu","family":"Liu","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Minhao","family":"Xie","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jianguo","family":"Lin","sequence":"additional","affiliation":[{"name":"NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063,China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"965","reference":[{"key":"ref=1","doi-asserted-by":"publisher","first-page":"394","DOI":"10.3322\/caac.21492","volume":"68","author":"Bray F.","year":"2018","unstructured":"Bray F.; Ferlay J.; Soerjomataram I.; Siegel R.L.; Torre L.A.; Jemal A.; Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. 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