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To prevent self\u2010aggregation and avoid problems of phthalocyanine isomerization, two silicon phthalocyanines di\u2010substituted axially with erlotinib have been synthesized and fully characterized. These conjugates are present in monomeric form in various solvents as well as culture media. Cell\u2010based experiments showed that these conjugates localize in lysosomes and mitochondria, while maintaining high photodynamic activities (IC<jats:sub>50<\/jats:sub> values as low as 8\u2005n<jats:sc>m<\/jats:sc> under a light dose of 1.5\u2005J\u2009cm<jats:sup>\u22122<\/jats:sup>). With erlotinib as the targeting moiety, two conjugates were found to exhibit high specificity for EGFR\u2010overexpressing cancer cells. Various poly(ethylene glycol) (PEG) linker lengths were shown to have an effect on the photophysical\/photochemical properties and on in\u2005vitro phototoxicity.<\/jats:p>","DOI":"10.1002\/cmdc.201700384","type":"journal-article","created":{"date-parts":[[2017,8,4]],"date-time":"2017-08-04T07:26:31Z","timestamp":1501831591000},"page":"1504-1511","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Silicon Phthalocyanines Axially Disubstituted with Erlotinib toward Small\u2010Molecular\u2010Target\u2010Based Photodynamic Therapy"],"prefix":"10.1002","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9148-2206","authenticated-orcid":false,"given":"Juan\u2010Juan","family":"Chen","sequence":"first","affiliation":[{"name":"National &amp; Local Joint Biomedical Engineering Research Center on Photodynamic Technologies, and Fujian Engineering Research Center of Functional Materials, College of Chemistry Fuzhou University  Fuzhou 350116 China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yi\u2010Zhen","family":"Huang","sequence":"additional","affiliation":[{"name":"National &amp; Local Joint Biomedical Engineering Research Center on Photodynamic Technologies, and Fujian Engineering Research Center of Functional Materials, College of Chemistry Fuzhou University  Fuzhou 350116 China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mei\u2010Ru","family":"Song","sequence":"additional","affiliation":[{"name":"National &amp; Local Joint Biomedical Engineering Research Center on Photodynamic Technologies, and Fujian Engineering Research Center of Functional Materials, College of Chemistry Fuzhou University  Fuzhou 350116 China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zhi\u2010Hong","family":"Zhang","sequence":"additional","affiliation":[{"name":"Fuzhou General Hospital of Nanjing Military Command  Fuzhou 350005 China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jin\u2010Ping","family":"Xue","sequence":"additional","affiliation":[{"name":"National &amp; Local Joint Biomedical Engineering Research Center on Photodynamic Technologies, and Fujian Engineering Research Center of Functional Materials, College of Chemistry Fuzhou University  Fuzhou 350116 China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2017,9,6]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrc1071"},{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrc1894"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr900300p"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1039\/C6CS00442C"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.chemrev.5b00244"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1039\/9781847551658"},{"key":"e_1_2_7_7_1","volume-title":"Sensitizers for Photodynamic Therapy: Phthalocyanines, Vol.\u20052","author":"Brasseur N.","year":"2003"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ccr.2010.05.002"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules17010098"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1039\/C5OB01035G"},{"key":"e_1_2_7_11_1","first-page":"1970","volume":"61","author":"Vrouenraets M. 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