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Bisphosphonates inhibit breast and prostate carcinoma cell invasion, an early event in the formation of bone metastases.
The molecular mechanisms by which tumor cells metastasize to bone are likely to involve invasion, cell adhesion to bone, and the release of soluble mediators from tumor cells that stimulateExpand
The relationship between the chemistry and biological activity of the bisphosphonates.
The ability of bisphosphonates ((HO)(2)P(O)CR(1)R(2)P(O)(OH)(2)) to inhibit bone resorption has been known since the 1960s, but it is only recently that a detailed molecular understanding of theExpand
Bisphosphonates inhibit prostate and breast carcinoma cell adhesion to unmineralized and mineralized bone extracellular matrices.
The molecular mechanisms by which tumor cells induce osteolytic metastases are likely to involve tumor cell adhesion to bone as well as the release of soluble mediators from tumor cells thatExpand
Long-term treatment with bisphosphonates and their safety in postmenopausal osteoporosis
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,Expand
Molecular Characterization of a Novel Geranylgeranyl Pyrophosphate Synthase from Plasmodium Parasites*
We present here a study of a eukaryotic trans-prenylsynthase from the malaria pathogen Plasmodium vivax. Based on the results of biochemical assays and contrary to previous indications, this enzymeExpand
Visualizing mineral binding and uptake of bisphosphonate by osteoclasts and non-resorbing cells.
Bisphosphonates (BPs) target bone due to their high affinity for calcium ions. During osteoclastic resorption, these drugs are released from the acidified bone surface and taken up by osteoclasts,Expand
Antiresorptive dose-response relationships across three generations of bisphosphonates.
The first generation of bisphosphonates was discovered in the late 1960s and is characterized by short alkyl or halide side-chains. Well known representatives of this class areExpand
Inhibition of Protein Prenylation by Bisphosphonates Causes Sustained Activation of Rac, Cdc42, and Rho GTPases
N‐BPs, which inhibit bone resorption by preventing prenylation of small GTPases, unexpectedly cause the accumulation of GTP‐bound, unprenylated Rho family GTPases in macrophages and osteoclasts. InExpand
Differentiating the mechanisms of antiresorptive action of nitrogen containing bisphosphonates.
Bisphosphonates (BPS) inhibit bone resorption and are divided into two classes according to their chemical structure and mechanism of action: nonnitrogen containing BPS such as etidronate andExpand
Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo.
Nitrogen-containing bisphosphonate drugs such as risedronate act by inhibiting farnesyl diphosphate synthase, thereby disrupting protein prenylation in osteoclasts. We recently found that anExpand
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