Thirty years of HDAC inhibitors: 2020 insight and hindsight
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 …
(HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory …
HDAC6 as privileged target in drug discovery: A perspective
Abstract HDAC6, a class IIB HDAC isoenzyme, stands unique in its structural and
physiological functions. Besides histone modification, largely due to its cytoplasmic …
physiological functions. Besides histone modification, largely due to its cytoplasmic …
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 …
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …
Recent advances in the discovery of potent and selective HDAC6 inhibitors
XX Wang, RZ Wan, ZP Liu - European journal of medicinal chemistry, 2018 - Elsevier
Histone deacetylase HDAC6, a member of the class IIb HDAC family, is unique among
HDAC enzymes in having two active catalytic domains, and has unique physiological …
HDAC enzymes in having two active catalytic domains, and has unique physiological …
Recent progress in histone deacetylase inhibitors as anticancer agents
Histone Deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that
play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis …
play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis …
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 …
several non-oncological conditions, such as inflammation and neurodegenerative disorders …
The search for potent, small‐molecule HDACIs in cancer treatment: a decade after vorinostat
Histone deacetylases (HDACs) play a crucial role in the remodeling of chromatin, and are
involved in the epigenetic regulation of gene expression. In the last decade, inhibition of …
involved in the epigenetic regulation of gene expression. In the last decade, inhibition of …
Development of first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools for dual inhibition of tubulin deacetylation
L Sinatra, A Vogelmann, F Friedrich… - Journal of medicinal …, 2023 - ACS Publications
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6
(HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration …
(HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration …
Drugging the HDAC6–HSP90 interplay in malignant cells
OH Krämer, S Mahboobi, A Sellmer - Trends in pharmacological sciences, 2014 - cell.com
Acetylation and deacetylation cycles regulate crucial biological processes. The enzymes
deacetylating lysine residues are termed histone deacetylases (HDACs). Eighteen …
deacetylating lysine residues are termed histone deacetylases (HDACs). Eighteen …
Histone deacetylase 8 (HDAC8) and its inhibitors with selectivity to other isoforms: An overview
The histone deacetylases (HDACs) enzymes provided crucial role in transcriptional
regulation of cells through deacetylation of nuclear histone proteins. Discoveries related to …
regulation of cells through deacetylation of nuclear histone proteins. Discoveries related to …