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Inhibition of TACC3 by a small molecule inhibitor in breast cancer

Loredana Campo1, Eun-Kyoung Breuer1

  • 1Department of Radiation Oncology, Stritch School of Medicine, Loyola University Chicago, Maywood, IL 60153, USA.

Biochemical and Biophysical Research Communications
|March 21, 2018
PubMed

Insights

Transforming acidic coiled-coil protein 3 (TACC3) inhibition by KHS101 suppresses breast cancer growth and stemness. This TACC3 inhibitor also reduces key mitotic kinases, suggesting dual targeting potential for breast cancer therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cell Biology

Background:

  • Transforming acidic coiled-coil protein 3 (TACC3) is linked to human cancers, including breast cancer.
  • High TACC3 levels in breast cancer correlate with DNA damage and sensitivity to radiation and PARP inhibitors.
  • The therapeutic potential of targeting TACC3 in breast cancer remains underexplored.

Purpose of the Study:

  • To investigate the therapeutic potential of the small molecule TACC3 inhibitor, KHS101, in breast cancer.
  • To elucidate the mechanisms underlying KHS101's action in breast cancer cells.
  • To explore KHS101's potential as a multi-targeting agent.

Main Methods:

  • Treatment of breast cancer cells with KHS101.
  • Assessment of cell growth, motility, epithelial-mesenchymal transition (EMT), stemness, and apoptosis.
  • Quantitative multiplexed proteomic analysis using tandem mass tags (TMTs).

Main Results:

  • KHS101 suppressed breast cancer cell growth, motility, EMT, and stemness, while inducing apoptosis.
  • Proteomic analysis revealed KHS101 affects multiple signaling pathways.
  • KHS101 significantly reduced the expression of mitotic kinases Aurora A and Polo-like kinase 1 (PLK1).

Conclusions:

  • KHS101 demonstrates significant anti-cancer effects in breast cancer models.
  • KHS101's mechanism involves the downregulation of TACC3 and associated mitotic kinases.
  • KHS101 shows promise as a novel therapeutic agent and potential dual/multi-targeting mitotic inhibitor for breast cancer treatment.
Keywords:
Cancer cell stemnessEMTKHS101Quantitative multiplexed proteomic analysisTACC3

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