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 …

The chemical biology of reversible lysine post-translational modifications

ZA Wang, PA Cole - Cell chemical biology, 2020 - cell.com
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …

Pathological role of HDAC8: cancer and beyond

JY Kim, H Cho, J Yoo, GW Kim, YH Jeon, SW Lee… - Cells, 2022 - mdpi.com
Histone deacetylase 8 (HDAC8) is a class I HDAC that catalyzes the deacetylation of histone
and non-histone proteins. As one of the best-characterized isoforms, numerous studies have …

Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: A review

R Sarkar, S Banerjee, SA Amin, N Adhikari… - European journal of …, 2020 - Elsevier
Abstract Among different Histone deacetylases (HDACs), histone deacetylase 3 (HDAC3) is
an epigenetic drug target which is currently marked as a potential therapeutic strategy to …

Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)

J Chotitumnavee, Y Yamashita, Y Takahashi… - Chemical …, 2022 - pubs.rsc.org
We developed a first-in-class proteolysis targeting chimera (PROTAC) for selective
degradation of histone deacetylase 8 (HDAC8). The PROTAC induced degradation of …

A genetically encoded, phage‐displayed cyclic‐peptide library

XS Wang, PHC Chen, JT Hampton… - Angewandte …, 2019 - Wiley Online Library
Superior to linear peptides in biological activities, cyclic peptides are considered to have
great potential as therapeutic agents. To identify cyclic‐peptide ligands for therapeutic …

CRISPR/dCas9 tools: Epigenetic mechanism and application in gene transcriptional regulation

R Cai, R Lv, X Shi, G Yang, J Jin - International Journal of Molecular …, 2023 - mdpi.com
CRISPR/Cas9-mediated cleavage of DNA, which depends on the endonuclease activity of
Cas9, has been widely used for gene editing due to its excellent programmability and …

Dissecting histone deacetylase 3 in multiple disease conditions: selective inhibition as a promising therapeutic strategy

N Adhikari, T Jha, B Ghosh - Journal of Medicinal Chemistry, 2021 - ACS Publications
The acetylation of histone and non-histone proteins has been implicated in several disease
states. Modulation of such epigenetic modifications has therefore made histone …

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 …

Targeting the E2F1/Rb/HDAC1 axis with the small molecule HR488B effectively inhibits colorectal cancer growth

N Duan, X Hu, H Qiu, R Zhou, Y Li, W Lu, Y Zhu… - Cell Death & …, 2023 - nature.com
Colorectal cancer (CRC), the third most common cancer worldwide, remains highly lethal as
the disease only becomes symptomatic at an advanced stage. Growing evidence suggests …