Endocrine Unit, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts 02114, USA.
J Biol Chem. 2013 Jul 12;288(28):20122-34. doi: 10.1074/jbc.M112.441360. Epub 2013 Jun 2.
Parathyroid hormone (PTH) is the only Food and Drug Administration-approved anabolic agent to treat osteoporosis; however, the cellular targets of PTH action in bone remain controversial. PTH modulates bone turnover by binding to the PTH/PTH-related peptide (PTHrP) type 1 receptor (PPR), a G-protein-coupled receptor highly expressed in bone and kidneys. Osteocytes, the most abundant cells in adult bone, also express PPR. However, the physiological relevance of PPR signaling in osteocytes remains to be elucidated. Toward this goal, we generated mice with PPR deletion in osteocytes (Ocy-PPRKO). Skeletal analysis of these mice revealed a significant increase in bone mineral density and trabecular and cortical bone parameters. Osteoblast activities were reduced in these animals, as demonstrated by decreased collagen type I α1 mRNA and receptor activator of NF-κB ligand (RANKL) expression. Importantly, when subjected to an anabolic or catabolic PTH regimen, Ocy-PPRKO animals demonstrated blunted skeletal responses. PTH failed to suppress SOST/Sclerostin or induce RANKL expression in Ocy-PPRKO animals compared with controls. In vitro, osteoclastogenesis was significantly impaired in Ocy-PPRKO upon PTH administration, indicating that osteocytes control osteoclast formation through a PPR-mediated mechanism. Taken together, these data indicate that PPR signaling in osteocytes is required for bone remodeling, and receptor signaling in osteocytes is needed for anabolic and catabolic skeletal responses.
甲状旁腺激素(PTH)是唯一获得美国食品和药物管理局批准用于治疗骨质疏松症的合成代谢药物;然而,PTH 在骨骼中的作用的细胞靶点仍存在争议。PTH 通过与甲状旁腺素/甲状旁腺素相关肽(PTHrP)1 型受体(PPR)结合来调节骨转换,PPR 是一种在骨骼和肾脏中高度表达的 G 蛋白偶联受体。成骨细胞,即成人骨骼中最丰富的细胞,也表达 PPR。然而,成骨细胞中 PPR 信号的生理相关性仍有待阐明。为了实现这一目标,我们生成了成骨细胞中 PPR 缺失的小鼠(Ocy-PPRKO)。这些小鼠的骨骼分析显示骨密度和小梁骨及皮质骨参数显著增加。这些动物的成骨细胞活性降低,表现为Ⅰ型胶原 α1 mRNA 和核因子 κB 受体激活剂配体(RANKL)表达减少。重要的是,当给予合成代谢或分解代谢 PTH 治疗时,Ocy-PPRKO 动物的骨骼反应减弱。与对照组相比,PTH 未能抑制 Ocy-PPRKO 动物的 SOST/Sclerostin 或诱导 RANKL 表达。在体外,给予 PTH 后 Ocy-PPRKO 中的破骨细胞生成明显受损,表明成骨细胞通过 PPR 介导的机制控制破骨细胞的形成。综上所述,这些数据表明成骨细胞中的 PPR 信号对于骨重塑是必需的,并且成骨细胞中的受体信号对于合成代谢和分解代谢的骨骼反应是必需的。