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Photodynamic cell-kill analysis of breast tumor cells with a tamoxifen-pyropheophorbide conjugate
Authors:Fernandez Gacio Ana  Fernandez-Marcos Carlos  Swamy Narasimha  Dunn Darra  Ray Rahul
Institution:Bioorganic Chemistry and Structural Biology, Section in Endocrinology, Diabetes and Metabolism, Department of Medicine, Boston University School of Medicine, Boston, Massachusetts 02118, USA.
Abstract:We hypothesized that estrogen receptor (ER) in hormone-sensitive breast cancer cells could be targeted for selective photodynamic killing of tumor cell with antiestrogen-porphyrin conjugates by combining the over-expression of ER in hormone-sensitive breast cancer cells and tumor-retention property of porphyrin photosensitizers. In this study we describe that a tamoxifen (TAM)-pyropheophorbide conjugate that specifically binds to ER alpha, caused selective cell-kill in MCF-7 breast cancer cells upon light exposure. Therefore, it is a potential candidate for ER-targeted photodynamic therapy of cancers (PDT) of tissues and organs that respond to estrogens/antiestrogens.
Keywords:estrogen receptor targeted delivery of phototoxins  tamoxifen‐porphyrin conjugate  photodynamic cell‐kill  breast cancer
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