Osteoporosis is a progressive bone disorder characterised by imbalance between bone building (anabolism) and resorption (catabolism). Most therapeutics target inhibition of osteoclast-mediated bone resorption, but more recent attention in early drug discovery has focussed on anabolic targets in osteoblasts or their precursors. Two marketed agents that display anabolic properties, strontium ranelate and teriparatide, mediate their actions via the G protein-coupled calcium-sensing and parathyroid hormone-1 receptors, respectively. This review explores their activity, the potential for improved therapeutics targeting these receptors and other putative anabolic GPCR targets, including Smoothened, Wnt/Frizzled, relaxin family peptide, adenosine, cannabinoid, prostaglandin and sphingosine-1-phosphate receptors.

骨质疏松症是一种进行性骨疾病，其特征在于骨骼形成（合成代谢）和吸收（分解代谢）之间不平衡。大多数治疗方法的目标是抑制破骨细胞介导的骨吸收，但在早期药物发现中，最近的注意力集中在成骨细胞或其前体的合成代谢目标上。两种具有合成代谢特性的市售试剂，雷奈酸锶和特立帕肽，分别通过G蛋白偶联的钙敏感受体和甲状旁腺激素1受体介导其作用。这篇综述探讨了它们的活性，以及​​针对这些受体和其他推定的合成代谢GPCR靶标的改良治疗方法的潜力，这些靶标包括Smoothened，Wnt / Frizzled，松弛素家族肽，腺苷，大麻素，前列腺素和鞘氨醇-1-磷酸受体。