Synthesis and estrogen receptor binding affinity of a porphyrin-estradiol conjugate for targeted photodynamic therapy of cancer.
A tetraphenylporphyrin-C11-beta-estradiol conjugate has been synthesized. Competitive binding assay of the conjugate with estrogen receptor (ER)-ligand-binding domain showed that the conjugate binds specifically to the protein with high affinity. Potential use of this conjugate to selectively deliver cytotoxic porphyrins to ER-positive cells in various carcinomas is discussed.
James
D A
DA
Department of Medicine, Boston University School of Medicine, MA 02118, USA.
Swamy
N
N
Paz
N
N
Hanson
R N
RN
Ray
R
R
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002417:Cattle; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use; D005260:Female; D006801:Humans; D010051:Ovarian Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010778:Photochemotherapy; D011166:Porphyrins / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000378:metabolism*; D013050:Spectrometry, Fluorescence; D014407:Tumor Cells, Cultured
C121727:11-(((4-(5,10,15-triphenylporphyrin-20-yl)phenyl)carbonylamino)butanoyloxy)estradiol; D011166:Porphyrins; D011960:Receptors, Estrogen; D004958:Estradiol