Department of Anatomy, Cell Biology & Physiology, Indiana University School of Medicine, Indianapolis, Indiana, USA.
Department of Orthopaedic Surgery, School of Medicine, UC Davis Health, Sacramento, California, USA.
J Bone Miner Res. 2023 May;38(5):765-774. doi: 10.1002/jbmr.4798. Epub 2023 Mar 22.
The development of Wnt-based osteoanabolic agents has progressed rapidly in recent years, given the potent effects of Wnt modulation on bone homeostasis. Simultaneous pharmacologic inhibition of the Wnt antagonists sclerostin and Dkk1 can be optimized to create potentiated effects in the cancellous bone compartment. We looked for other candidates that might be co-inhibited along with sclerostin to potentiate the effects in the cortical compartment. Sostdc1 (Wise), like sclerostin and Dkk1, also binds and inhibits Lrp5/6 coreceptors to impair canonical Wnt signaling, but Sostdc1 has greater effects in the cortical bone. To test this concept, we deleted Sostdc1 and Sost from mice and measured the skeletal effects in cortical and cancellous compartments individually. Sost deletion alone produced high bone mass in all compartments, whereas Sostdc1 deletion alone had no measurable effects on either envelope. Mice with codeletion of Sostdc1 and Sost had high bone mass and increased cortical properties (bone mass, formation rates, mechanical properties), but only among males. Combined administration of sclerostin antibody and Sostdc1 antibody in wild-type female mice produced potentiation of cortical bone gain despite no effect of Sostdc1 antibody alone. In conclusion, Sostdc1 inhibition/deletion can work in concert with sclerostin deficiency to improve cortical bone properties. © 2023 The Authors. Journal of Bone and Mineral Research published by Wiley Periodicals LLC on behalf of American Society for Bone and Mineral Research (ASBMR).
近年来,基于 Wnt 的成骨激动剂的发展迅速,这是因为 Wnt 调节对骨稳态具有强大的作用。同时抑制 Wnt 拮抗剂骨硬化蛋白和 Dkk1 可以优化作用,增强松质骨部位的效果。我们寻找其他可能与骨硬化蛋白共同抑制的候选药物,以增强皮质骨部位的效果。Sostdc1(Wise)与骨硬化蛋白和 Dkk1 一样,也结合并抑制 Lrp5/6 核心受体,从而损害经典 Wnt 信号传导,但 Sostdc1 对皮质骨的作用更大。为了验证这一概念,我们在小鼠中敲除了 Sostdc1 和 Sost,并分别测量了皮质骨和松质骨部位的骨骼效应。单独敲除 Sost 会导致所有部位的骨量增加,而单独敲除 Sostdc1 则对任何部位都没有可测量的影响。Sostdc1 和 Sost 同时敲除的小鼠骨量增加,皮质骨特性(骨量、形成率、机械性能)增加,但仅在雄性中。在野生型雌性小鼠中联合给予骨硬化蛋白抗体和 Sostdc1 抗体可增强皮质骨的获得,尽管单独给予 Sostdc1 抗体没有效果。总之,Sostdc1 抑制/缺失可以与骨硬化蛋白缺乏协同作用,改善皮质骨特性。