Chetomin, targeting HIF-1α/p300 complex, exhibits antitumour activity in multiple myeloma

Elena Viziteu1, Camille Grandmougin1, Hartmut Goldschmidt2,3

  • 1Institute of Human Genetics, CNRS-UPR1142, Montpellier F-34396, France.

British Journal of Cancer
|February 12, 2016
PubMed
Abstract

Insights

Chetomin, a HIF-1α/p300 inhibitor, shows anti-cancer effects in multiple myeloma (MM). This compound may benefit MM patients with high EP300/HIF-1α expression and poor prognosis.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Multiple myeloma (MM) is a fatal plasma cell cancer.
  • Constitutive hypoxia-inducible factor 1-alpha (HIF-1α) expression in MM indicates HIF-1α-mediated transcription as a potential therapeutic target.

Purpose of the Study:

  • To investigate the therapeutic potential of targeting the HIF-1α/p300 interaction in multiple myeloma.

Main Methods:

  • Disruption of the HIF-1α/p300 co-activator complex to inhibit HIF transcriptional activity.
  • Utilizing chetomin, a known inhibitor of the HIF-1α/p300 interaction.

Main Results:

  • Chetomin demonstrated significant anti-tumour activity.
  • This activity was observed in both human myeloma cell lines and primary MM cells from patients.

Conclusions:

  • Chetomin exhibits potential clinical value for treating multiple myeloma.
  • It may be particularly effective for patients with high EP300/HIF-1α expression and a poor prognosis.

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