Colletta A A, Wakefield L M, Howell F V, Danielpour D, Baum M, Sporn M B
Department of Surgery, Kings College School of Medicine and Dentistry, Rayne Institute, London, United Kingdom.
J Clin Invest. 1991 Jan;87(1):277-83. doi: 10.1172/JCI114983.
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.
最近的实验研究确定了合成孕激素孕二烯酮(Gestodene)的一个新的细胞内结合位点,该位点似乎在人乳腺癌细胞中独特表达。本文显示,孕二烯酮以剂量依赖的方式抑制人乳腺癌细胞的生长,但对内分泌反应性人子宫内膜癌细胞没有影响。孕二烯酮可使T47D人乳腺癌细胞分泌的转化生长因子-β(TGF-β)增加90倍。其他合成孕激素没有这种作用,这表明这种诱导作用是由新的孕二烯酮结合位点介导的,而不是由传统的孕酮受体介导的。此外,在四种乳腺癌细胞系中,TGF-β的诱导程度与孕二烯酮结合位点的细胞内水平相关。在缺乏孕二烯酮结合位点但表达高水平孕酮受体的子宫内膜癌细胞系HECl-B中,未观察到TGF-β的诱导。孕二烯酮对T47D细胞生长的抑制作用可被抗TGF-β多克隆抗血清部分逆转。这些数据表明,孕二烯酮的生长抑制作用可能部分是由TGF-β的自分泌诱导介导的。