Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite.
- G. H. Nancollas, R. Tang, F. Ebetino
- Biology, ChemistryBone
- 1 May 2006
Bisphosphonates inhibit breast and prostate carcinoma cell invasion, an early event in the formation of bone metastases.
- S. Boissier, M. Ferreras, P. Clézardin
- Biology, ChemistryCancer Research
- 1 June 2000
Evidence that BP pretreatment of breast and prostate carcinoma cells inhibited tumor cell invasion in a dose-dependent manner is provided and BPs may be useful agents for the prophylactic treatment of patients with cancers that are known to preferentially metastasize to bone is suggested.
The relationship between the chemistry and biological activity of the bisphosphonates.
- F. Ebetino, Anne-Marie L. Hogan, R. Russell
- Biology, ChemistryBone
- 1 July 2011
Long-term treatment with bisphosphonates and their safety in postmenopausal osteoporosis
- M. Pazianas, C. Cooper, F. Ebetino, R. Russell
- MedicineTherapeutics and Clinical Risk Management
- 21 July 2010
Bisphosphonates are the leading drugs for the treatment of osteoporosis. In randomized controlled trials (RCTs), alendronate, risedronate, and zoledronate have shown to reduce the risk of vertebral,…
Bisphosphonates inhibit prostate and breast carcinoma cell adhesion to unmineralized and mineralized bone extracellular matrices.
- S. Boissier, S. Magnetto, P. Clézardin
- Biology, MedicineCancer Research
- 15 September 1997
Evidence is provided for a direct cellular effect of BP in preventing tumor cell adhesion to bone, suggesting that BPs may be useful agents for the prophylactic treatment of patients with cancer that is known to preferentially metastasize to bone.
Inhibition of Protein Prenylation by Bisphosphonates Causes Sustained Activation of Rac, Cdc42, and Rho GTPases
- J. Dunford, M. Rogers, F. Ebetino, R. Phipps, F. Coxon
- Biology, ChemistryJournal of Bone and Mineral Research
- 1 May 2006
N‐BPs, which inhibit bone resorption by preventing prenylation of small GTPases, unexpectedly cause the accumulation of GTP‐bound, unprenylated Rho family GTPase in macrophages and osteoclasts, causing inappropriate activation of downstream signaling pathways.
Molecular Characterization of a Novel Geranylgeranyl Pyrophosphate Synthase from Plasmodium Parasites*
- J. Artz, A. Wernimont, R. Hui
- BiologyJournal of Biological Chemistry
- 17 November 2010
Structural analysis shows that the product length is constrained by a hydrophobic cavity formed primarily by a set of residues from the same subunit as the product as well as at least one other from the dimeric partner, and Plasmodium GGPP synthase (GGPPS) can bind nitrogen-containing bisphosphonates strongly with the energetically favorable cooperation of three Mg2+, resulting in inhibition by this class of compounds at IC50 concentrations below 100 nm.
Antiresorptive dose-response relationships across three generations of bisphosphonates.
- W. Sietsema, F. Ebetino, A. M. Salvagno, J. Bevan
- Chemistry, BiologyDrugs under experimental and clinical research
Many of the first-, second- and third-generation bisphosphonates have been tested in a model of retinoid-induced bone resorption, and in this model the rank ordering of potency is similar, though somewhat larger doses of bisph phosphonate are required to block the Resorption induced by the retinoids.
Visualizing mineral binding and uptake of bisphosphonate by osteoclasts and non-resorbing cells.
- F. Coxon, K. Thompson, A. Roelofs, F. Ebetino, M. Rogers
- Biology, MedicineBone
- 1 May 2008
Differences between bisphosphonates in binding affinities for hydroxyapatite.
- M. Lawson, Z. Xia, R. Russell
- BiologyJournal of Biomedical Materials Research. Part B…
There are substantial differences among BPs in their binding to HAP, which may be exploited in the development of biomaterials and may also partly explain the extent of their relative skeletal retention and persistence of biological effects observed in both animal and clinical studies.