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 …
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 …
[HTML][HTML] Histone deacetylase 11 is an ε-N-myristoyllysine hydrolase
C Moreno-Yruela, I Galleano, AS Madsen… - Cell chemical biology, 2018 - cell.com
Histone deacetylase (HDAC) enzymes regulate diverse biological function, including gene
expression, rendering them potential targets for intervention in a number of diseases, with a …
expression, rendering them potential targets for intervention in a number of diseases, with a …
Enriching proteolysis targeting chimeras with a second modality: When two are better than one
A Salerno, F Seghetti, J Caciolla, E Uliassi… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
Evolution of slow-binding inhibitors targeting histone deacetylase isoforms
Because the overexpression of histone deacetylase enzymes (HDACs) has been linked to
numerous diseases, including various cancers and neurodegenerative disorders, HDAC …
numerous diseases, including various cancers and neurodegenerative disorders, HDAC …
An update on the emerging approaches for histone deacetylase (HDAC) inhibitor drug discovery and future perspectives
M Su, X Gong, F Liu - Expert Opinion on Drug Discovery, 2021 - Taylor & Francis
Introduction HDACs catalyze the removal of acetyl groups from the ε-N-acetylated lysine
residues of various protein substrates including both histone and nonhistone proteins …
residues of various protein substrates including both histone and nonhistone proteins …
[HTML][HTML] Mechanism-based inhibitors of SIRT2: structure–activity relationship, X-ray structures, target engagement, regulation of α-tubulin acetylation and inhibition of …
Sirtuin 2 (SIRT2) is a protein deacylase enzyme that removes acetyl groups and longer
chain acyl groups from post-translationally modified lysine residues. It affects diverse …
chain acyl groups from post-translationally modified lysine residues. It affects diverse …
Determination of slow-binding HDAC inhibitor potency and subclass selectivity
C Moreno-Yruela, CA Olsen - ACS Medicinal Chemistry Letters, 2022 - ACS Publications
Histone deacetylases (HDACs) 1–3 regulate chromatin structure and gene expression.
These three enzymes are targets for cancer chemotherapy and have been studied for the …
These three enzymes are targets for cancer chemotherapy and have been studied for the …
[HTML][HTML] Resolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors
NC Payne, R Mazitschek - Cell Chemical Biology, 2022 - cell.com
The histone deacetylase paralogs HDAC1/2/3 and their corepressor complexes serve as
epigenetic master regulators of chromatin function. Over the past decades, HDACs have …
epigenetic master regulators of chromatin function. Over the past decades, HDACs have …
Direct peptide cyclization and one-pot modification using the MeDbz linker
The one-pot synthesis and modification of cyclic peptides through a self-cleaving on-resin
protocol is described. We apply Dawson's MeDbz linker to achieve direct intramolecular …
protocol is described. We apply Dawson's MeDbz linker to achieve direct intramolecular …