Photodynamic cell-kill analysis of breast tumor cells with a tamoxifen-pyropheophorbide conjugate.
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.
Fernandez Gacio
Ana
A
Bioorganic Chemistry and Structural Biology, Section in Endocrinology, Diabetes and Metabolism, Department of Medicine, Boston University School of Medicine, Boston, Massachusetts 02118, USA.
Fernandez-Marcos
Carlos
C
Swamy
Narasimha
N
Dunn
Darra
D
Ray
Rahul
R
D018931:Antineoplastic Agents, Hormonal / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor / Q000187:drug effects*; D002470:Cell Survival; D002734:Chlorophyll / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D047628:Estrogen Receptor alpha / Q000378:metabolism; D005260:Female; D006801:Humans; D015394:Molecular Structure; D010778:Photochemotherapy / Q000379:methods*; D011166:Porphyrins / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D018931:Antineoplastic Agents, Hormonal; D047628:Estrogen Receptor alpha; D011166:Porphyrins; D020845:Selective Estrogen Receptor Modulators; C520103:tamoxifen-pyropheophorbide conjugate; D013629:Tamoxifen; D002734:Chlorophyll; C040298:pyropheophorbide a