Introducing HDAC-targeting radiopharmaceuticals for glioblastoma imaging and therapy

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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.