Cellular and molecular mechanisms of action of bisphosphonates

M J Rogers, Sharon Andrea Gordon, H L Benford, Fraser Coxon, S P Luckman, J Monkkonen, J C Frith

Research output: Contribution to journalArticlepeer-review

877 Citations (Scopus)


Bisphosphonates currently are the most important class of antiresorptive agents used in the treatment of metabolic bone diseases, including tumor-associated osteolysis and hypercalcemia, Paget's disease, and osteoporosis. These compounds have high affinity for calcium and therefore target to bone mineral, where they appear to be internalized selectively by bone-resorbing osteoclasts and inhibit osteoclast function.
Original languageEnglish
Pages (from-to)2961-2978
Number of pages18
Issue number12
Publication statusPublished - 2000


  • Animals
  • Bone Resorption
  • Bone and Bones
  • Diphosphonates
  • Humans
  • Osteoblasts
  • Osteoclasts
  • Protein Prenylation
  • Protein Tyrosine Phosphatases
  • Proton-Translocating ATPases
  • Structure-Activity Relationship


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