Research Area: Metabolic Disease, Endocrinology
Biological Activity:
Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. It is a nitrogen-containing bisphosphate that acts as a robust inhibitor of bone resorption and induces apoptosis in osteoclasts. [1] It causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC50 = 460 nM). [2] It efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC50 ~ 40 - 70 µM). And it also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC50 ~ 1 pM, in vitro invasion of prostate cancer cells). |