Abstract
Recent experimental work has identified a novel intracellular binding site for the synthetic progestin, Gestodene, that appears to be uniquely expressed in human breast cancer cells. Gestodene is shown here to inhibit the growth of human breast cancer cells in a dose-dependent fashion, but has no effect on endocrine-responsive human endometrial cancer cells. Gestodene induced a 90-fold increase in the secretion of transforming growth factor-beta (TGF-beta) by T47D human breast cancer cells. Other synthetic progestins had no effect, indicating that this induction is mediated by the novel Gestodene binding site and not by the conventional progesterone receptor. Furthermore, in four breast cancer cell lines, the extent of induction of TGF-beta correlated with intracellular levels of Gestodene binding site. No induction of TGF-beta was observed with the endometrial cancer line, HECl-B, which lacks the Gestodene binding site, but which expresses high levels of progesterone receptor. The inhibition of growth of T47D cells by Gestodene is partly reversible by a polyclonal antiserum to TGF-beta. These data indicate that the growth-inhibitory action of Gestodene may be mediated in part by an autocrine induction of TGF-beta.
MeSH Terms
Binding Sites
Breast Neoplasms/metabolism,pathology
Cell Division/drug effects
Enzyme-Linked Immunosorbent Assay
Estrogen Antagonists/pharmacology
Female
Humans
Norpregnenes/metabolism,pharmacology
Progesterone Congeners/pharmacology
RNA, Messenger/analysis
Radioligand Assay
Receptors, Progesterone/analysis
Transforming Growth Factor beta/analysis,biosynthesis
Tumor Cells, Cultured
Chemicals
Estrogen Antagonists
Norpregnenes
Progesterone Congeners
RNA, Messenger
Receptors, Progesterone
Transforming Growth Factor beta
Gestodene
Authors & Affiliations
6 authors, click to expand affiliations / ORCID
Colletta A A
Department of Surgery, Kings College School of Medicine and Dentistry, Rayne Institute, London, United Kingdom.
Wakefield L M
Howell F V
Danielpour D
Baum M
Sporn M B
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