G protein-coupled receptors as anabolic drug targets in osteoporosis

Natalie Diepenhorst, Patricia Rueda, Anna E. Cook, Philippe Pastoureau, Massimo Sabatini, Christopher J. Langmead

Research output: Contribution to journalReview ArticleResearchpeer-review

8 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)1-12
Number of pages12
JournalPharmacology and Therapeutics
Publication statusPublished - 1 Apr 2018


  • Bone anabolism
  • Calcium-sensing receptor
  • Frizzled receptors
  • G protein-coupled receptors (GPCRs)
  • Osteoporosis
  • Parathyroid hormone receptor

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