title: Internalization of a C17α-alkynylestradiol-porphyrin conjugate into estrogen receptor positive MCF-7 breast cancer cells.
abstract: We hypothesized that expression of nuclear estrogen receptor (ER) in hormone-sensitive breast cancer cells could be harnessed synergistically with the tumor-accumulating effect of porphyrins to selectively deliver estrogen-porphyrin conjugates into breast tumor cells, and preferentially kill tumor cells upon exposure to visible light. In this study we synthesized a conjugate of C(17α)-alkynylestradiol and pyropheophorbide and demonstrated that this conjugate is internalized by ER-positive MCF-7 cells while pyropheophorbide did not, suggesting an ER-mediated uptake and internalization of the conjugate by incipient nuclear ER in MCF-7 cells. This study is a direct demonstration of our hypothesis about ER-mediated internalization of estrogen-porphyrin conjugates.
authors.affiliation: Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA, USA.
authors.forename: Sara
authors.initials: S
authors.lastname: Sadler
authors.forename: Kelly S
authors.initials: KS
authors.lastname: Persons
authors.forename: Graham B
authors.initials: GB
authors.lastname: Jones
authors.forename: Rahul
authors.initials: R
authors.lastname: Ray
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D002734:Chlorophyll / Q000031:analogs & derivatives* / Q000737:chemistry; D004958:Estradiol / Q000737:chemistry*; D005260:Female; D006801:Humans; D008856:Microscopy, Fluorescence; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D011960:Receptors, Estrogen / Q000378:metabolism*
chemical_list: D017319:Photosensitizing Agents; D011960:Receptors, Estrogen; D002734:Chlorophyll; C040298:pyropheophorbide a; D004958:Estradiol