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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.
Abstract:
Despite recent advances in multimodality therapy for glioblastoma (GB) incorporating surgery, radiotherapy, chemotherapy and targeted therapy, the overall prognosis remains poor. One of the interesting targets for GB therapy is the histone deacetylase family (HDAC). Due to their pleiotropic effects on, e.g., DNA repair, cell proliferation, differentiation, apoptosis and cell cycle, HDAC inhibitors have gained a lot of attention in the last decade as anti-cancer agents. Despite their known underlying mechanism, their therapeutic activity is not well-defined. In this review, an extensive overview is given of the current status of HDAC inhibitors for GB therapy, followed by an overview of current HDAC-targeting radiopharmaceuticals. Imaging HDAC expression or activity could provide key insights regarding the role of HDAC enzymes in gliomagenesis, thus identifying patients likely to benefit from HDACi-targeted therapy.
Insights
Histone deacetylase (HDAC) inhibitors show promise for glioblastoma (GB) therapy. This review explores HDAC inhibitors and radiopharmaceuticals for GB, highlighting imaging
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.
