Department of Pharmacology and Therapeutics, Centre for Research in Reproduction and Development, McGill University, Montreal, Quebec, Canada.
Endocrinology. 2019 Mar 1;160(3):675-683. doi: 10.1210/en.2018-01038.
Bone morphogenetic proteins (BMPs) are pleiotropic ligands in the TGF-β superfamily. In the early to mid-2000s, several BMPs, including BMP2, were shown to regulate FSH synthesis alone and in synergy with activins in immortalized gonadotrope-like cell lines and primary pituitary cultures. Activins are also TGF-β family members, which were identified and named based on their abilities to stimulate FSH production selectively. Mechanistic analyses suggested that BMP2 promoted expression of the FSHβ subunit gene (Fshb) via at least two nonmutually exclusive mechanisms. First, BMP2 stimulated the production of the inhibitor of DNA-binding proteins 1, 2, and 3 (Id1, Id2, and Id3), which potentiated the stimulatory actions of homolog of Drosophila mothers against decapentaplegic 3 (SMAD3) on the Fshb promoter. SMAD3 is an intracellular signaling protein that canonically mediates the actions of activins and is an essential regulator of Fshb production in vitro and in vivo. Second, BMP2 was shown to activate SMAD3-dependent signaling via its canonical type IA receptor, BMPR1A (also known as ALK3). This was a surprising result, as ALK3 conventionally activates distinct SMAD proteins. Although these initial results were compelling, they were challenged by contemporaneous and subsequent observations. For example, inhibitors of BMP signaling did not specifically impair FSH production in cultured pituitary cells. Of perhaps greater significance, mice lacking ALK3 in gonadotrope cells produced FSH normally. Therefore, the physiological role of BMPs in FSH synthesis in vivo is presently uncertain.
骨形态发生蛋白(BMPs)是 TGF-β 超家族中的多效配体。在 21 世纪初到中期,包括 BMP2 在内的几种 BMP 被证明可以单独调节 FSH 的合成,并与激活素在永生化的促性腺激素样细胞系和原代垂体培养物中协同作用。激活素也是 TGF-β 家族成员,它们的名称和功能是基于它们选择性刺激 FSH 产生的能力。机制分析表明,BMP2 通过至少两种非相互排斥的机制促进 FSHβ亚基基因(Fshb)的表达。首先,BMP2 刺激 DNA 结合蛋白 1、2 和 3(Id1、Id2 和 Id3)的抑制剂的产生,这增强了同源物果蝇母体对抗 decapentaplegic 3(SMAD3)对 Fshb 启动子的刺激作用。SMAD3 是一种细胞内信号蛋白,经典地介导激活素的作用,并且是体外和体内 Fshb 产生的必需调节剂。其次,BMP2 通过其经典的 IA 型受体 BMPR1A(也称为 ALK3)激活 SMAD3 依赖性信号。这是一个令人惊讶的结果,因为 ALK3 通常激活不同的 SMAD 蛋白。尽管这些最初的结果令人信服,但它们受到了同时期和随后的观察结果的挑战。例如,BMP 信号抑制剂不会特异性地损害培养的垂体细胞中的 FSH 产生。也许更重要的是,ALK3 缺失的小鼠在促性腺激素细胞中正常产生 FSH。因此,BMPs 在体内 FSH 合成中的生理作用目前尚不确定。