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 …
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 deacetylation. Aberrant expression of HDACs is associated with various human …
First-in-class hydrazide-based HDAC6 selective inhibitor with potent oral anti-inflammatory activity by attenuating NLRP3 inflammasome activation
K Yue, S Sun, G Jia, M Qin, X Hou… - Journal of Medicinal …, 2022 - ACS Publications
In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-
binding group (ZBG), which displays superior pharmacokinetic properties to the current …
binding group (ZBG), which displays superior pharmacokinetic properties to the current …
Discovery of HDAC6, HDAC8, and 6/8 inhibitors and development of cell-based drug screening models for the treatment of TGF-β-induced idiopathic pulmonary …
WC Yu, TY Yeh, CH Ye, PCT Chong… - Journal of Medicinal …, 2023 - ACS Publications
Idiopathic pulmonary fibrosis is incurable, and its progression is difficult to control and thus
can lead to pulmonary deterioration. Pan-histone deacetylase inhibitors such as SAHA have …
can lead to pulmonary deterioration. Pan-histone deacetylase inhibitors such as SAHA have …
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 …
A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019)
S Shen, AP Kozikowski - Expert opinion on therapeutic patents, 2020 - Taylor & Francis
ABSTRACT Introduction: Histone deacetylase 6 (HDAC6) is unique in comparison with other
zinc-dependent HDAC family members. An increasing amount of evidence from clinical and …
zinc-dependent HDAC family members. An increasing amount of evidence from clinical and …
Discovery of a new isoxazole-3-hydroxamate-based histone deacetylase 6 inhibitor SS-208 with antitumor activity in syngeneic melanoma mouse models
S Shen, M Hadley, K Ustinova, J Pavlicek… - Journal of medicinal …, 2019 - ACS Publications
Isoxazole is a five-membered heterocycle that is widely used in drug discovery endeavors.
Here, we report the design, synthesis, and structural and biological characterization of SS …
Here, we report the design, synthesis, and structural and biological characterization of SS …
Non-hydroxamate zinc-binding groups as warheads for histone deacetylases
A Frühauf, FJ Meyer-Almes - Molecules, 2021 - mdpi.com
Histone deacetylases (HDACs) remove acetyl groups from acetylated lysine residues and
have a large variety of substrates and interaction partners. Therefore, it is not surprising that …
have a large variety of substrates and interaction partners. Therefore, it is not surprising that …
Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors
MT Tavares, AP Kozikowski, S Shen - European journal of medicinal …, 2021 - Elsevier
Abstract Histone deacetylase 6 (HDAC6) is a zinc-dependent HDAC that mainly modulates
the acetylation status of non-histone substrates, such as α-tubulin and heat shock protein 90 …
the acetylation status of non-histone substrates, such as α-tubulin and heat shock protein 90 …
Histone deacetylase inhibitor based prodrugs
W Fan, L Zhang, Q Jiang, W Song, F Yan… - European Journal of …, 2020 - Elsevier
Histone deacetylases (HDACs) are a family of enzymes which play important roles in the
development and progression of cancers. Inhibition of HDACs has been widely studied as a …
development and progression of cancers. Inhibition of HDACs has been widely studied as a …