Martin T J, Sims N A, Ng K W
St Vincent's Institute of Medical Research, Melbourne, Australia.
Osteoporos Int. 2008 Aug;19(8):1125-38. doi: 10.1007/s00198-008-0575-5. Epub 2008 Mar 13.
The understanding of cell interactions and genetic controls of bone cells has provided new approaches to drug development for osteoporosis. Current emphasis in the development of new anabolic therapies is directed at modifying the effects of Wnt signalling on osteoblast differentiation and bone formation. Local signalling that results in bone formation during remodelling takes place in several ways. Growth factors released from resorbed bone matrix can contribute to preosteoblast differentiation and bone formation. Osteoclasts in the bone multicellular units (BMUs) might also generate activity that contributes to bone formation. The preosteoblasts themselves, growing in the resorption space, can communicate through cell contact and paracrine signalling mechanisms to differentiate. Osteocytes can sense the need for bone repair by detecting damage and pressure changes, and signalling to surface cells to respond appropriately. These recent insights into cell communication, together with discoveries from human and mouse genetics, have opened new pathways to drug development for osteoporosis. With the anabolic effect of parathyroid hormone on the skeleton having been established, human genetics revealed the major role of Wnt signalling in bone formation, and this has become the target of activity. Current approaches include activation at any of several points in the Wnt pathway, and neutralization of sclerostin, the protein product of the SOST gene that is produced in osteocytes as a powerful inhibitor of bone formation.
对骨细胞间相互作用和基因调控的理解为骨质疏松症的药物研发提供了新途径。目前新型促合成疗法的研发重点在于改变Wnt信号对成骨细胞分化和骨形成的影响。重塑过程中导致骨形成的局部信号传导通过多种方式发生。从吸收的骨基质中释放的生长因子可促进前成骨细胞分化和骨形成。骨多细胞单元(BMU)中的破骨细胞也可能产生有助于骨形成的活性。在吸收空间中生长的前成骨细胞自身可通过细胞接触和旁分泌信号机制进行通讯以实现分化。骨细胞可通过检测损伤和压力变化来感知骨修复的需求,并向表面细胞发出信号以做出适当反应。这些对细胞通讯的最新见解,以及来自人类和小鼠遗传学的发现,为骨质疏松症的药物研发开辟了新途径。随着甲状旁腺激素对骨骼的促合成作用得到证实,人类遗传学揭示了Wnt信号在骨形成中的主要作用,这已成为研究热点。目前的方法包括在Wnt通路的多个位点进行激活,以及中和骨硬化蛋白,即SOST基因的蛋白质产物,它在骨细胞中作为一种强大的骨形成抑制剂产生。