Structural basis for the regulation of nucleosome recognition and HDAC activity by histone deacetylase assemblies

JH Lee, D Bollschweiler, T Schäfer, R Huber - Science Advances, 2021 - science.org
The chromatin-modifying histone deacetylases (HDACs) remove acetyl groups from acetyl-
lysine residues in histone amino-terminal tails, thereby mediating transcriptional repression …

Tetrahydroquinoline-capped histone deacetylase 6 inhibitor SW-101 ameliorates pathological phenotypes in a Charcot–Marie–Tooth type 2A mouse model

S Shen, C Picci, K Ustinova, V Benoy… - Journal of Medicinal …, 2021 - ACS Publications
Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of
neurodegenerative disorders. SW-100 (1a), a phenylhydroxamate-based HDAC6 inhibitor …

Role of fluorination in the histone deacetylase 6 (HDAC6) selectivity of benzohydroxamate-based inhibitors

G Sandrone, CD Cukier, K Zrubek… - ACS Medicinal …, 2021 - ACS Publications
Nonselective histone deacetylase (HDAC) inhibitors show dose-limiting side effects due to
the inhibition of multiple, essential HDAC subtypes that can be limited or prevented by …

[HTML][HTML] A Novel Class of Schistosoma mansoni Histone Deacetylase 8 (HDAC8) Inhibitors Identified by Structure-Based Virtual Screening and In Vitro Testing

CV Simoben, D Robaa, A Chakrabarti, K Schmidtkunz… - Molecules, 2018 - mdpi.com
A promising means in the search of new small molecules for the treatment of
schistosomiasis (amongst other parasitic ailments) is by targeting the parasitic epigenome …

[HTML][HTML] Acetylated α-Tubulin and α-Synuclein: physiological interplay and contribution to α-synuclein oligomerization

AM Calogero, MJ Basellini, HB Isilgan… - International Journal of …, 2023 - mdpi.com
Emerging evidence supports that altered α-tubulin acetylation occurs in Parkinson's disease
(PD), a neurodegenerative disorder characterized by the deposition of α-synuclein fibrillary …

Discovery of 1, 2, 4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy

Z Yang, M Shen, M Tang, W Zhang, X Cui… - European journal of …, 2019 - Elsevier
In this study, a series of novel HDAC inhibitors, using 1, 2, 4-oxadiazole-containing as the
cap group, were synthesized and evaluated in vitro. Compound 14b, N-hydroxy-2-(methyl …

Structure, functions and selective inhibitors of HDAC6

T Liang, H Fang - Current Topics in Medicinal Chemistry, 2018 - ingentaconnect.com
Histone deacetylases 6 (HDAC6) has emerged as a promising target for the treatment of
various human diseases including cancer, neurodegenerative disease and immunology due …

Multitarget approach for the treatment of Alzheimer's disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) covering diverse …

O Rabal, JA Sánchez-Arias… - ACS chemical …, 2019 - ACS Publications
Here, we present a series of dual-target phosphodiesterase 9 (PDE9) and histone
deacetylase (HDAC) inhibitors devised as pharmacological tool compounds for assessing …

[HTML][HTML] Crystal structure of histone deacetylase 6 complexed with (R)-lipoic acid, an essential cofactor in central carbon metabolism

PR Watson, JG Stollmaier, DW Christianson - Journal of Biological …, 2023 - ASBMB
The enzyme cofactor (R)-lipoic acid plays a critical role in central carbon metabolism due to
its catalytic function in the generation of acetyl-CoA, which links glycolysis with the …

Dual targeting strategies on histone deacetylase 6 (HDAC6) and heat shock protein 90 (Hsp90)

D Bonanni, A Citarella, D Moi, L Pinzi… - Current medicinal …, 2022 - ingentaconnect.com
The design of multi-target drugs acting simultaneously on multiple signaling pathways is a
growing field in medicinal chemistry, especially for the treatment of complex diseases, such …