F H Ebetino

TL;DR: Each bisphosphonates has a unique profile that may help to explain potential clinical differences among them, in terms of their speed and duration of action, and effects on fracture reduction.

TL;DR: The potency of a wider range of nitrogen-containing bisphosphonates, including the highly potent, heterocycle-containing zoledronic acid and minodronate, is examined, finding a clear correlation between the ability to inhibit farnesyl diphosphate synthase in vitro, and to inhibit protein prenylation in cell-free extracts and in purified osteoclasts in vitro and in vivo.

TL;DR: The observed differences in kinetic binding affinities, HAP zeta potentials, and interfacial tension are likely to contribute to the biological properties of the various bisphosphonates and may contribute to differences in uptake and persistence in bone and the reversibility of effects.

TL;DR: 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.

TL;DR: High-resolution x-ray structures of the human enzyme in complexes with risedronate and zoledronate, two of the leading N-BPs in clinical use, reveal the molecular binding characteristics of an important pharmacological target and provide a route for further optimization of these important drugs.