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Inhibitors of human farnesyl pyrophosphate synthase (hFPPS), such as risedronate (Actonel) and zoledronate (Zometa), are therapeutically used to treat osteoporosis and bone cancer. Currently, almost all of them share a common bisphosphonate moiety which is the major contributor to their non-selective binding to hFPPS, as well as other related enzymes. These highly polar molecules exhibit low oral bioavailability and high accumulation into bone tissue. Our goal is to design more selective inhibitors with significantly reduced dependency on a bisphosphonate moiety for binding into the active site of hFPPS. A structure-based approach has been pursued in designing novel inhibitors of hFPPS, …
