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JTC-801 exerts anti-proliferative effects in human osteosarcoma cells by inducing apoptosis

Chang-Jun Zheng1, Li-Li Yang2, Jun Liu3

  • 1a Department of Orthopaedics , The 2nd Hospital of Jilin University , Changchun , PR China.

Journal of Receptor and Signal Transduction Research
|February 16, 2018
PubMed
Abstract

Insights

JTC-801, a G protein-coupled receptor (GPCR) antagonist, inhibits osteosarcoma cell growth by inducing apoptosis and reducing cell invasion. It also impacts the PI3K/AKT signaling pathway, offering potential for cancer therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are key targets for drug discovery.
  • Novel agents are needed to inhibit cancer cell proliferation and induce apoptosis.
  • JTC-801 is a novel GPCR antagonist with potential antitumor effects.

Purpose of the Study:

  • Investigate the antitumor effects of JTC-801 on human osteosarcoma cells (U2OS).
  • Elucidate the underlying mechanisms of JTC-801's action in osteosarcoma.

Main Methods:

  • Cell Counting Kit-8 assay for cell viability.
  • Flow cytometry with Annexin V-FITC/PI for apoptosis evaluation.
  • Transwell assays for invasion and migration.
  • Western blot for protein level analysis.

Main Results:

  • JTC-801 significantly decreased U2OS cell viability and induced apoptosis by activating BAX and Caspase-3, while down-regulating BCL-2.
  • JTC-801 treatment reduced cell invasion and migration.
  • JTC-801 inhibited the PI3K/AKT signaling pathway by reducing phosphorylated AKT, mTOR, and active p70 S6 kinase.

Conclusions:

  • JTC-801 exhibits antitumor effects against osteosarcoma cells.
  • JTC-801 promotes apoptosis and inhibits proliferation and metastasis.
  • The PI3K/AKT signaling pathway is involved in JTC-801's mechanism of action.
Keywords:
BCL-2 familyJTC-801PI3K/AKT signaling pathwayapoptosisosteosarcomaproliferation

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