Introducing HDAC-targeting radiopharmaceuticals for glioblastoma imaging and therapy
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Date
Authors
Everix, Liesbeth
Seane, Elsie Neo
Ebenhan, Thomas
Goethals, Ingeborg
Bolcaen, Julie
Journal Title
Journal ISSN
Volume Title
Publisher
MDPI
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.
Description
SUPPLEMENTARY MATERIALS : TABLE S1: Representative summary of the preclinical development for candidate HDACi-derived glioma therapy.
Keywords
Glioblastoma, Histone deacetylases inhibitors, Radiopharmaceuticals, Theranostics, SDG-03: Good health and well-being
Sustainable Development Goals
SDG-03:Good heatlh and well-being
Citation
Everix, L.; Seane, E.N.;
Ebenhan, T.; Goethals, I.; Bolcaen, J.
Introducing HDAC-Targeting
Radiopharmaceuticals for
Glioblastoma Imaging and Therapy.
Pharmaceuticals 2023, 16, 227.
https://DOI.org/10.3390/ph16020227.