Anticancer therapy with HDAC inhibitors: mechanism-based combination strategies and future perspectives

R Jenke, N Reßing, FK Hansen, A Aigner, T Büch - Cancers, 2021 - mdpi.com
Simple Summary Beyond mutations, epigenetic changes have been described as drivers for
cancer as well. While leaving the overall DNA structure intact, they can be responsible for …

Combining histone deacetylase inhibitors (HDACis) with other therapies for cancer therapy

M Zhou, M Yuan, M Zhang, C Lei, O Aras… - European journal of …, 2021 - Elsevier
Histone deacetylases (HDACs) play an important role in regulating the expression of genes
involved in tumorigenesis and tumor maintenance, and hence they have been considered …

Current trends in development of HDAC-based chemotherapeutics

N Cheshmazar, M Hamzeh-Mivehroud, HN Charoudeh… - Life Sciences, 2022 - Elsevier
Abstract Background Histone deacetylases (HDACs) are one of the essential epigenetic
targets in cancer treatment. These enzymes play key roles in post-translation modification …

The application of PROTAC in HDAC

S Chen, Y Zheng, B Liang, Y Yin, J Yao, Q Wang… - European journal of …, 2023 - Elsevier
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great
opportunities for scientific research and industrial applications. Histone deacetylase (HDAC) …

Molecular hybridization: a powerful tool for multitarget drug discovery

P de Sena Murteira Pinheiro, LS Franco… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction The current drug discovery paradigm of 'one drug, multiple targets' has gained
attention from both the academic medicinal chemistry community and the pharmaceutical …

[HTML][HTML] CUDC907, a dual phosphoinositide-3 kinase/histone deacetylase inhibitor, promotes apoptosis of NF2 Schwannoma cells

J Huegel, CT Dinh, M Martinelli, O Bracho, R Rosario… - Oncotarget, 2022 - ncbi.nlm.nih.gov
Abstract Neurofibromatosis Type 2 (NF2) is a rare tumor disorder caused by pathogenic
variants of the merlin tumor suppressor encoded by NF2. Patients develop vestibular …

Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells

J Deng, B Hou, X Hou, Y Chen, T Zhang… - European Journal of …, 2023 - Elsevier
Inhibition of PI3K and histone deacetylase (HDAC) activity simultaneously using a single
molecule appears to be a promising approach for cancer treatment. Current PI3K/HDAC …

[HTML][HTML] Discovery of first novel sigma/HDACi dual-ligands with a potent in vitro antiproliferative activity

C Barbaraci, V di Giacomo, A Maruca, V Patamia… - Bioorganic …, 2023 - Elsevier
Designing and discovering compounds for dual-target inhibitors is challenging to synthesize
new, safer, and more efficient drugs than single-target drugs, especially to treat multifactorial …

Challenges and discoveries in polypharmacology of neurodegenerative diseases

TCM Lustoza Rodrigues, NF de Sousa… - Current Topics in …, 2023 - ingentaconnect.com
Background: Neurological disorders are composed of several diseases that affect the central
and peripheral nervous system; among these are neurodegenerative diseases, which lead …

Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors

Y Duan, T Yu, L Jin, S Zhang, X Shi, Y Zhang… - European Journal of …, 2023 - Elsevier
Histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1) are attractive
targets for epigenetic cancer therapy. There is an intimate interplay between the two …