Fernandez Gacio Ana, Fernandez-Marcos Carlos, Swamy Narasimha, Dunn Darra, Ray Rahul
Bioorganic Chemistry and Structural Biology, Section in Endocrinology, Diabetes and Metabolism, Department of Medicine, Boston University School of Medicine, Boston, Massachusetts 02118, USA.
J Cell Biochem. 2006 Oct 15;99(3):665-70. doi: 10.1002/jcb.20932.
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.
我们推测,通过结合激素敏感性乳腺癌细胞中雌激素受体(ER)的过表达以及卟啉光敏剂的肿瘤滞留特性,抗雌激素 - 卟啉共轭物可靶向激素敏感性乳腺癌细胞中的雌激素受体,用于选择性光动力杀伤肿瘤细胞。在本研究中,我们描述了一种与ERα特异性结合的他莫昔芬(TAM)- 焦脱镁叶绿酸共轭物,光照后在MCF - 7乳腺癌细胞中引起选择性细胞杀伤。因此,它是对雌激素/抗雌激素有反应的组织和器官的ER靶向光动力治疗癌症(PDT)的潜在候选物。