Bisphosphonates used for the treatment of bone disorders inhibit squalene synthase and cholesterol biosynthesis.

@article{Amin1992BisphosphonatesUF,
  title={Bisphosphonates used for the treatment of bone disorders inhibit squalene synthase and cholesterol biosynthesis.},
  author={Dilip Amin and Sonia A Cornell and Shelley Gustafson and Saul J. Needle and John W Ullrich and Glenda E. Bilder and Mark H. Perrone},
  journal={Journal of lipid research},
  year={1992},
  volume={33 11},
  pages={1657-63}
}
Some bisphosphonates used for the treatment of bone disorders are also potent inhibitors of squalene synthase, a critical enzyme for sterol biosynthesis. Among seven drugs tested, YM 175 (cycloheptylaminomethylene-1,1-bisphosphonic acid) was the most potent inhibitor of rat liver microsomal squalene synthase (Ki = 57 nM) and sterol biosynthesis from [14C]mevalonate in rat liver homogenate (IC50 = 17 nM). EB 1053 (3-(1-pyrolidino)-1-hydroxypropylidene-1,1-bisphosphonic acid) and PHPBP (3-(1… CONTINUE READING

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