HDAC6 as privileged target in drug discovery: A perspective

S Pulya, SA Amin, N Adhikari, S Biswas, T Jha… - Pharmacological …, 2021 - Elsevier
Abstract HDAC6, a class IIB HDAC isoenzyme, stands unique in its structural and
physiological functions. Besides histone modification, largely due to its cytoplasmic …

A review of progress in histone deacetylase 6 inhibitors research: structural specificity and functional diversity

XH Zhang, Qin-Ma, HP Wu, MY Khamis… - Journal of medicinal …, 2021 - ACS Publications
Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing
histone deacetylation. Aberrant expression of HDACs is associated with various human …

Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)

C Zhao, H Dong, Q Xu, Y Zhang - Expert opinion on therapeutic …, 2020 - Taylor & Francis
Introduction: Histone deacetylase (HDAC) inhibitors play a crucial role in restoring the
balance of acetylation and deacetylation of lysine residues of histones and non-histone …

Strategies to design selective histone deacetylase inhibitors

J Melesina, CV Simoben, L Praetorius… - …, 2021 - Wiley Online Library
This review classifies drug‐design strategies successfully implemented in the development
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …

Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinants

M Marek, TB Shaik, T Heimburg… - Journal of medicinal …, 2018 - ACS Publications
Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that
represent promising therapeutic targets for the treatment of numerous human diseases. Yet …

Hydroxamic acid derivatives: From synthetic strategies to medicinal chemistry applications

A Citarella, D Moi, L Pinzi, D Bonanni, G Rastelli - ACS omega, 2021 - ACS Publications
Since the approval of three hydroxamic acid-based HDAC inhibitors as anticancer drugs,
such functional groups acquired even more notoriety in synthetic medicinal chemistry. The …

Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)

Y Li, S Sang, W Ren, Y Pei, Y Bian, Y Chen… - European journal of …, 2021 - Elsevier
Alzheimer's disease (AD) is one of the most common neurodegenerative disorders, which is
characterized by the primary risk factor, age. Several attempts have been made to treat AD …

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 …

Synthesis and biological investigation of phenothiazine-based benzhydroxamic acids as selective histone deacetylase 6 inhibitors

K Vögerl, N Ong, J Senger, D Herp… - Journal of medicinal …, 2019 - ACS Publications
The phenothiazine system was identified as a favorable cap group for potent and selective
histone deacetylase 6 (HDAC6) inhibitors. Here, we report the preparation and systematic …

Structure, mechanism, and inhibition of the zinc-dependent histone deacetylases

NJ Porter, DW Christianson - Current opinion in structural biology, 2019 - Elsevier
Zinc-dependent histone deacetylases (HDACs) regulate the biological function of histone
and non-histone proteins through the hydrolysis of acetyllysine side chains to yield free …