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Published TCIMAIL newest issue No.197
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Bone Resorption Inhibitor
No.159(October 2013)
Bisphosphonates (BPs), including alendronate, ibandronate, etc., are very effective inhibitors of bone resorption in vivo and in vitro. Disodium tiludronate (1) is one of the BPs. These compounds are characterized by two C-P bonds which are located on the same carbon atom, i.e. geminal BPs, and have been used in many research projects regarding bone metabolism.
According to differences in the side chain, BPs can be divided into two groups, non-nitrogen containing BPs and nitrogen-containing BPs. The former can be metabolized to methylene-containing analogues of ATP (AppCp) and the metabolite causes osteoclast cell death. The latter can inhibit farnesyl pyrophosphate synthetase in the mevalonate biosynthetic pathway. 1 is a non-nitrogen containing BP and compound 2 is the AppCp from 1. For detailed information, please refer to the following references.1-5)
References
- 1)Bisphosphonates: Mechanisms of action
- 2)Bisphosphonates: From bench to bedside
- 3)Bisphosphonates: Mode of action and pharmacology
- 4)Computational insights into binding of bisphosphates to farnesyl pyrophosphate synthase
- 5)Biochemical and molecular mechanisms of action of bisphosphonates
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