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

Aya Yamamura1, Md Junayed Nayeem1, Motohiko Sato1

  • 1Department of Physiology, Aichi Medical University, 1-1 Yazakokarimata, Nagakute, Aichi, 480-1195, Japan.

Journal of Pharmacological Sciences
|February 28, 2019
PubMed

Insights

Calcilytics, Ca2+-sensing receptor antagonists, inhibit prostate cancer cell proliferation and migration. These compounds also down-regulate CaSR expression, indicating potential as novel prostate cancer therapeutics.

Area of Science:

  • Oncology
  • Molecular Pharmacology
  • Cell Biology

Background:

  • Prostate cancer development involves dysregulated calcium (Ca2+) signaling.
  • The Ca2+-sensing receptor (CaSR) plays a role in cancer cell physiology.
  • Targeting CaSR presents a potential therapeutic strategy for prostate cancer.

Purpose of the Study:

  • To investigate the pharmacological effects of CaSR antagonists (calcilytics) on human prostate cancer cells.
  • To evaluate the impact of calcilytics on cell proliferation, migration, and CaSR expression.

Main Methods:

  • Utilized human prostate cancer PC-3 cells.
  • Administered CaSR antagonists NPS2143 and Calhex 231.
  • Assessed cytosolic Ca2+ levels, cell proliferation (IC50), and cell migration.
  • Measured CaSR protein expression levels.

Main Results:

  • NPS2143 and Calhex 231 effectively blocked extracellular Ca2+-induced Ca2+ influx.
  • Calcilytics significantly inhibited PC-3 cell proliferation and migration.
  • Exposure to NPS2143 or Calhex 231 led to decreased CaSR protein expression.

Conclusions:

  • Calcilytics demonstrate anti-proliferative and anti-migratory effects in prostate cancer cells.
  • These compounds down-regulate CaSR expression in prostate cancer.
  • Calcilytics show promise as potential novel therapeutic agents for prostate cancer treatment.
Keywords:
CalcilyticCalcium-sensing receptorProstate cancer

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