G protein-coupled receptors (GPCRs) coupled to activation of Gs, such as the PTH1 receptor (PTH1R), have long been known to regulate skeletal function and homeostasis. However, the role of GPCRs coupled to other G proteins such as Gi is not well established. We used the tet-off system to regulate the expression of an activated Gi-coupled GPCR (Ro1) in osteoblasts in vivo. Skeletal phenotypes were assessed in mice expressing Ro1 from conception, from late stages of embryogenesis, and after weaning. Long bones were assessed histologically and by microcomputed tomography. Expression of Ro1 from conception resulted in neonatal lethality that was associated with reduced bone mineralization. Expression of Ro1 starting at late embryogenesis resulted in a severe trabecular bone deficit at 12 wk of age (>51% reduction in trabecular bone volume fraction in the proximal tibia compared with sex-matched control littermates; n = 11; P < 0.01). Ro1 expression for 8 wk beginning at 4 wk of age resulted in a more than 20% reduction in trabecular bone volume fraction compared with sex-matched control littermates (n = 16; P < 0.01). Bone histomorphometry revealed that Ro1 expression is associated with reduced rates of bone formation and mineral apposition without a significant change in osteoblast or osteoclast surface. Our results indicate that signaling by a Gi-coupled GPCR in osteoblasts leads to osteopenia resulting from a reduction in trabecular bone formation. The severity of the phenotype is related to the timing and duration of Ro1 expression during growth and development. The skeletal phenotype in Ro1 mice bears some similarity to that produced by knockout of Gs-alpha expression in osteoblasts and thus may be due at least in part to Gi-mediated inhibition of adenylyl cyclase.

译文

g蛋白偶联受体 (GPCRs) 与Gs的激活 (例如PTH1受体 (PTH1R)) 偶联,长期以来一直已知可以调节骨骼功能和体内平衡。但是,与其他g蛋白 (例如Gi) 偶联的GPCRs的作用尚不明确。我们使用tet-off系统调节体内成骨细胞中活化的Gi偶联GPCR (Ro1) 的表达。在受孕,胚胎发生后期和断奶后表达Ro1的小鼠中评估了骨骼表型。通过组织学和显微计算机断层扫描对长骨进行评估。受孕后Ro1的表达导致新生儿致死,这与骨矿化减少有关。在胚胎发生晚期开始的Ro1的表达导致在12周龄时严重的小梁骨缺损 (与性别匹配的同窝对照相比,胫骨近端的小梁骨体积分数> 51% 减少; n = 11; P <0.01)。与性别匹配的同窝对照组相比,从4周龄开始的8周Ro1表达导致小梁骨体积分数减少20% 以上 (n = 16; P <0.01)。骨组织形态计量学显示,Ro1表达与骨形成和矿物质并置率降低有关,而成骨细胞或破骨细胞表面没有明显变化。我们的结果表明,成骨细胞中Gi偶联GPCR的信号传导导致骨小梁骨形成减少导致骨质减少。表型的严重程度与生长发育过程中Ro1表达的时间和持续时间有关。Ro1小鼠的骨骼表型与成骨细胞中Gs-α 表达的敲除产生的表型相似,因此可能至少部分归因于Gi介导的腺苷酸环化酶的抑制。

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