Department of Physiology and Breast Cancer and the Environment Research Center, Michigan State University, East Lansing, Michigan 48824, USA.
Endocrinology. 2012 Oct;153(10):4990-5001. doi: 10.1210/en.2012-1518. Epub 2012 Aug 21.
Mammary organoids from adult mice produce tubules, analogous to mammary ducts in vivo, in response to hepatocyte growth factor (HGF) when cultured in collagen gels. The combination of HGF plus progestin (R5020) causes reduced tubule number and length. We hypothesized that the inhibitory effect on tubulogenesis was due to progestin-mediated alteration of HGF/c-Met signaling. Using molecular inhibitors and short hairpin RNA, it was determined that HGF activation of Ras-related C3 botulinum toxin substrate (Rac1) was required for the formation of cytoplasmic extensions, the first step of tubulogenesis, and that Rac1 activity was Src kinase (Src) and focal adhesion kinase (FAK) dependent. The highly novel finding was that R5020 reduced tubulogenesis by up-regulating and increasing extracellular laminin and α6-integrin ligation to reduce activation of the Src, focal adhesion kinase, and Rac1 pathway. Receptor activator of nuclear factor-κB ligand, another progesterone-induced paracrine factor, did not replicate this effect of R5020. The inhibitory effect of R5020 on tubulogenesis was likely mediated through progesterone receptor (PR) isoform A (PRA), because PRA is the predominant PR isoform expressed in the organoids, and the progestin-induced effect was prevented by the PR antagonist RU486. These results provide a plausible mechanism that explains progestin/PRA-mediated blunting of HGF-induced tubulogenesis in vitro and is proposed to be relevant to progesterone/PRA-induced side-branching in vivo during pregnancy.
当在胶原蛋白凝胶中培养时,来自成年小鼠的乳腺类器官对肝细胞生长因子(HGF)做出反应,生成类似于体内乳腺导管的小管。HGF 与孕激素(R5020)联合使用会导致小管数量和长度减少。我们假设对小管生成的抑制作用是由于孕激素介导的 HGF/c-Met 信号转导改变所致。使用分子抑制剂和短发夹 RNA,确定 HGF 对 Ras 相关 C3 肉毒杆菌毒素底物(Rac1)的激活是细胞质延伸形成的必需条件,细胞质延伸是小管生成的第一步,并且 Rac1 活性依赖Src 激酶(Src)和粘着斑激酶(FAK)。一个非常新颖的发现是,R5020 通过上调和增加细胞外层粘连蛋白和α6-整合素连接来减少 Src、粘着斑激酶和 Rac1 通路的激活,从而减少小管生成。核因子-κB 配体受体激活剂(另一种孕激素诱导的旁分泌因子)并没有复制 R5020 的这种作用。R5020 对小管生成的抑制作用可能是通过孕激素受体(PR)亚型 A(PRA)介导的,因为 PRA 是类器官中表达的主要 PR 亚型,而 PR 拮抗剂 RU486 可阻止孕激素诱导的作用。这些结果提供了一个合理的机制,解释了孕激素/PRA 介导的 HGF 诱导的小管生成在体外的钝化,并且据推测与孕激素/PRA 诱导的妊娠期间体内侧支分支有关。