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Epidermal Growth Factor Receptor-Targeted Multifunctional Photosensitizers for Bladder Cancer Imaging and Photodynamic Therapy

Title
Epidermal Growth Factor Receptor-Targeted Multifunctional Photosensitizers for Bladder Cancer Imaging and Photodynamic Therapy
Authors
Cheruku, Ravindra R.Cacaccio, JosephDurrani, Farukh A.Tabaczynski, Walter A.Watson, RamonaMarko, AimeeKumar, RahulEl-Khouly, Mohamed E.Fukuzumi, ShunichiMissert, Joseph R.Yao, RutaoSajjad, MunawwarChandra, DhyanGuru, KhurshidPandey, Ravindra K.
Ewha Authors
Shunichi Fukuzumi
SCOPUS Author ID
Shunichi Fukuzumiscopus
Issue Date
2019
Journal Title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0022-2623JCR Link

1520-4804JCR Link
Citation
JOURNAL OF MEDICINAL CHEMISTRY vol. 62, no. 5, pp. 2598 - 2617
Publisher
AMER CHEMICAL SOC
Indexed
SCI; SCIE; SCOPUS WOS
Document Type
Article
Abstract
The in vitro and in vivo anticancer activity of iodinated photosensitizers (PSs) with and without an erlotinib moiety was investigated in UMUC3 [epidermal growth factor (EGFR)-positive] and T24 (EGFR-low) cell lines and tumored mice. Both the erlotinib-conjugated PSs 3 and 5 showed EGFR target specificity, but the position-3 erlotinib-PS conjugate 3 demonstrated lower photodynamic therapy efficacy than the corresponding non-erlotinib analogue 1, whereas the conjugate 5 containing an erlotinib moiety at position-17 of the PS showed higher tumor uptake and long-term tumor cure (severe combined immunodeficient mice bearing UMUC3 tumors). PS-erlotinib conjugates in the absence of light were ineffective in vitro and in vivo, but robust apoptotic and necrotic cell death was observed in bladder cancer cells after exposing them to a laser light at 665 nm. In contrast to F-18-fluorodeoxyglucose, a positron emission tomography agent, the position-17 erlotinib conjugate (I-124-analogue 6) showed enhanced UMUC3 tumor contrast even at a low imaging dose of 15 mu Ci/mouse.
DOI
10.1021/acs.jmedchem.8b01927
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자연과학대학 > 화학·나노과학전공 > Journal papers
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