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Introducing HDAC-Targeting Radiopharmaceuticals for Glioblastoma Imaging and Therapy.

Liesbeth Everix1, Elsie Neo Seane2, Thomas Ebenhan3,4,5

  • 1Molecular Imaging Center Antwerp (MICA), University of Antwerp, 2610 Antwerpen, Belgium.

Pharmaceuticals (Basel, Switzerland)
|June 1, 2023
PubMed
Summary

Histone deacetylase (HDAC) inhibitors show promise for glioblastoma (GB) therapy. This review explores HDAC inhibitors and radiopharmaceuticals for GB, highlighting imaging

Keywords:
glioblastomahistone deacetylases inhibitorsradiopharmaceuticalstheranostics

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Area of Science:

  • Oncology
  • Molecular Biology
  • Radiopharmaceuticals

Background:

  • Glioblastoma (GB) remains a challenging brain cancer with poor prognosis despite multimodal treatments.
  • Histone deacetylases (HDACs) are emerging targets due to their role in cell proliferation, apoptosis, and DNA repair.
  • HDAC inhibitors (HDACi) are investigated as anti-cancer agents, but their therapeutic efficacy in GB requires further definition.

Purpose of the Study:

  • To provide a comprehensive review of the current status of HDAC inhibitors in glioblastoma therapy.
  • To overview existing HDAC-targeting radiopharmaceuticals for glioblastoma.
  • To explore the potential of imaging HDAC expression or activity for patient stratification and therapeutic guidance.

Main Methods:

  • Literature review of preclinical and clinical studies on HDAC inhibitors for glioblastoma.
  • Survey of current developments in HDAC-targeting radiopharmaceuticals.
  • Discussion of the role of HDAC imaging in gliomagenesis and treatment selection.

Main Results:

  • HDAC inhibitors exhibit pleiotropic effects relevant to cancer therapy, including DNA repair and cell cycle regulation.
  • The therapeutic activity of HDAC inhibitors in glioblastoma is not yet fully elucidated.
  • Radiopharmaceuticals targeting HDACs are being developed for imaging and potentially therapeutic applications.

Conclusions:

  • HDAC inhibitors represent a promising therapeutic strategy for glioblastoma.
  • HDAC-targeting radiopharmaceuticals offer potential for non-invasive assessment of HDAC activity.
  • Imaging HDAC expression could identify glioblastoma patients who may benefit from HDAC inhibitor therapy.