Thirty years of HDAC inhibitors: 2020 insight and hindsight

TCS Ho, AHY Chan, A Ganesan - Journal of medicinal chemistry, 2020 - ACS Publications
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …

Dietary and physiological effects of zinc on the immune system

I Wessels, HJ Fischer, L Rink - Annual review of nutrition, 2021 - annualreviews.org
Evidence for the importance of zinc for all immune cells and for mounting an efficient and
balanced immune response to various environmental stressors has been accumulating in …

Comprehensive Mechanistic View of the Hydrolysis of Oxadiazole-Based Inhibitors by Histone Deacetylase 6 (HDAC6)

L Motlová, I Šnajdr, Z Kutil, E Andris… - ACS Chemical …, 2023 - ACS Publications
Histone deacetylase (HDAC) inhibitors used in the clinic typically contain a hydroxamate
zinc-binding group (ZBG). However, more recent work has shown that the use of alternative …

The zinc-binding group effect: lessons from non-hydroxamic acid vorinostat analogs

S Geurs, D Clarisse, K De Bosscher… - Journal of Medicinal …, 2023 - ACS Publications
Histone deacetylases (HDACs) are enzymes pursued as drug targets in various cancers and
several non-oncological conditions, such as inflammation and neurodegenerative disorders …

Potent hydrazide-based HDAC inhibitors with a superior pharmacokinetic profile for efficient treatment of acute myeloid leukemia in vivo

Y Jiang, J Xu, K Yue, C Huang, M Qin… - Journal of Medicinal …, 2021 - ACS Publications
As “Michael acceptors” may induce promiscuous responses in mammalian cells by reacting
with various proteins, we modified the cinnamamide of our previous hydrazide-based HDAC …

A therapeutic perspective of HDAC8 in different diseases: an overview of selective inhibitors

A Fontana, I Cursaro, G Carullo, S Gemma… - International Journal of …, 2022 - mdpi.com
Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional
repression and chromatin condensation mechanisms by removing the acetyl moiety from …

[HTML][HTML] HDACs and the epigenetic plasticity of cancer cells: Target the complexity

C Brancolini, T Gagliano, M Minisini - Pharmacology & therapeutics, 2022 - Elsevier
Cancer cells must adapt to the hostile conditions of the microenvironment in terms of
nutrition, space, and immune system attack. Mutations of DNA are the drivers of the …

[HTML][HTML] Novel epigenetic therapeutic strategies and targets in cancer

Q Babar, A Saeed, TA Tabish, S Pricl, H Townley… - … et Biophysica Acta (BBA …, 2022 - Elsevier
The critical role of dysregulated epigenetic pathways in cancer genesis, development, and
therapy has typically been established as a result of scientific and technical innovations in …

Mechanism of assembly, activation and lysine selection by the SIN3B histone deacetylase complex

MSM Wan, R Muhammad, MG Koliopoulos… - Nature …, 2023 - nature.com
Lysine acetylation in histone tails is a key post-translational modification that controls
transcription activation. Histone deacetylase complexes remove histone acetylation, thereby …

Silicon switch: Carbon–silicon Bioisosteric replacement as a strategy to modulate the selectivity, physicochemical, and drug‐like properties in anticancer …

J Fotie, CM Matherne… - Chemical Biology & Drug …, 2023 - Wiley Online Library
Bioisosterism is one of the leading strategies in medicinal chemistry for the design and
modification of drugs, consisting in replacing an atom or a substituent with a different atom or …