Calcilytics inhibit the proliferation and migration of human prostate cancer PC-3 cells.

The carcinogenesis and development of prostate cancer are mediated by enhanced Ca2+ signaling. In the present study, the pharmacological profile of the Ca2+-sensing receptor (CaSR) antagonists (calcilytics) was examined in human prostate cancer PC-3 cells. NPS2143 and Calhex 231 blocked extracellular Ca2+-induced increases in cytosolic [Ca2+]. NPS2143 and Calhex 231 inhibited cell proliferation (IC50 = 7.4 and 10.3 μM, respectively) and migration. The exposure to NPS2143 or Calhex 231 down-regulated CaSR protein expression. These results demonstrated that calcilytics inhibited cell proliferation/migration and down-regulated CaSR expression in human prostate cancer cells, suggesting their potential as novel therapeutic drugs for prostate cancer.