St. Vincent's Institute of Medical Research, Fitzroy, Victoria, Australia.
The University of Melbourne, Department of Medicine at St. Vincent's Hospital, Fitzroy, Victoria, Australia.
J Bone Miner Res. 2018 Jan;33(1):137-153. doi: 10.1002/jbmr.3291. Epub 2017 Oct 3.
Parathyroid hormone-related protein (PTHrP) and parathyroid hormone (PTH) have N-terminal domains that bind a common receptor, PTHR1. N-terminal PTH (teriparatide) and now a modified N-terminal PTHrP (abaloparatide) are US Food and Drug Administration (FDA)-approved therapies for osteoporosis. In physiology, PTHrP does not normally circulate at significant levels, but acts locally, and osteocytes, cells residing within the bone matrix, express both PTHrP and the PTHR1. Because PTHR1 in osteocytes is required for normal bone resorption, we determined how osteocyte-derived PTHrP influences the skeleton. We observed that adult mice with low PTHrP in osteocytes (targeted with the Dmp1(10kb)-Cre) have low trabecular bone volume and osteoblast numbers, but osteoclast numbers were unaffected. In addition, bone size was normal, but cortical bone strength was impaired. Osteocyte-derived PTHrP therefore stimulates bone formation and bone matrix strength, but is not required for normal osteoclastogenesis. PTHrP knockdown and overexpression studies in cultured osteocytes indicate that osteocyte-secreted PTHrP regulates their expression of genes involved in matrix mineralization. We determined that osteocytes secrete full-length PTHrP with no evidence for secretion of lower molecular weight forms containing the N-terminus. We conclude that osteocyte-derived full-length PTHrP acts through both PTHR1 receptor-mediated and receptor-independent actions in a paracrine/autocrine manner to stimulate bone formation and to modify adult cortical bone strength. © 2017 American Society for Bone and Mineral Research.
甲状旁腺激素相关蛋白 (PTHrP) 和甲状旁腺激素 (PTH) 具有结合共同受体 PTHR1 的 N 端结构域。N 端 PTH(特立帕肽)和现在经过修饰的 N 端 PTHrP(abaloparatide)是美国食品和药物管理局 (FDA) 批准用于治疗骨质疏松症的疗法。在生理学中,PTHrP 通常不会以显著水平循环,而是在局部起作用,而位于骨基质内的骨细胞表达 PTHrP 和 PTHR1。因为骨细胞中的 PTHR1 是正常骨吸收所必需的,所以我们确定了骨细胞来源的 PTHrP 如何影响骨骼。我们观察到,骨细胞中 PTHrP 水平较低的成年小鼠(用 Dmp1(10kb)-Cre 靶向)具有较低的小梁骨体积和成骨细胞数量,但破骨细胞数量不受影响。此外,骨大小正常,但皮质骨强度受损。因此,骨细胞来源的 PTHrP 刺激骨形成和骨基质强度,但不是正常破骨细胞生成所必需的。在培养的骨细胞中进行的 PTHrP 敲低和过表达研究表明,骨细胞分泌的 PTHrP 调节其参与基质矿化的基因表达。我们确定骨细胞分泌全长的 PTHrP,没有证据表明分泌含有 N 端的较低分子量形式。我们得出结论,骨细胞来源的全长 PTHrP 通过 PTHR1 受体介导和受体非依赖的旁分泌/自分泌方式发挥作用,以刺激骨形成并改变成年皮质骨强度。© 2017 美国骨矿研究协会。