Inside HDACs with more selective HDAC inhibitors

J Roche, P Bertrand - European journal of medicinal chemistry, 2016 - Elsevier
Inhibitors of histone deacetylases (HDACs) are nowadays part of the therapeutic arsenal
mainly against cancers, with four compounds approved by the Food and Drug …

HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors

R Sangwan, R Rajan, PK Mandal - European journal of medicinal chemistry, 2018 - Elsevier
Even though one is moving towards the success in the discovery of efficient anti-cancer
molecules, the drugs used in the treatment of various malignancies are found to possess …

[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 …

β-Peptoid foldamers at last

JS Laursen, J Engel-Andreasen… - Accounts of Chemical …, 2015 - ACS Publications
Conspectus For a long time, peptides were considered unsuitable for drug development due
to their inherently poor pharmacokinetic properties and proteolytic susceptibility. However …

[HTML][HTML] Innovative strategies for selective inhibition of histone deacetylases

AR Maolanon, AS Madsen, CA Olsen - Cell chemical biology, 2016 - cell.com
Histone deacetylases (HDAC) are a family of closely related enzymes involved in epigenetic
and posttranscriptional regulation of numerous genes and proteins. Their deregulation is …

[HTML][HTML] Histone deacetylase inhibitors from marine invertebrates

C Luparello, M Mauro, V Arizza, M Vazzana - Biology, 2020 - mdpi.com
Simple Summary Histone deacetylases (HDACs) are enzymes that control gene expression
and are involved in the onset of serious human pathologies, including cancer; hence, their …

Histone deacetylase 3 inhibitors in learning and memory processes with special emphasis on benzamides

SA Amin, N Adhikari, S Kotagiri, T Jha… - European Journal of …, 2019 - Elsevier
Among numerous essential processes, memory and learning are important work of the
brain. Epigenetic manipulations through histone acetyltransferases (HATs) and histone …

Natural and synthetic macrocyclic inhibitors of the histone deacetylase enzymes

AR Maolanon, HME Kristensen, LJ Leman… - …, 2017 - Wiley Online Library
Inhibition of histone deacetylase (HDAC) enzymes has emerged as a target for development
of cancer chemotherapy. Four compounds have gained approval for clinical use by the Food …

Design, multicomponent synthesis, and anticancer activity of a focused histone deacetylase (HDAC) inhibitor library with peptoid-based cap groups

V Krieger, A Hamacher, CGW Gertzen… - Journal of medicinal …, 2017 - ACS Publications
In this work, we report the multicomponent synthesis of a focused histone deacetylase
(HDAC) inhibitor library with peptoid-based cap groups and different zinc-binding groups. All …

Chemical editing of macrocyclic natural products and kinetic profiling reveal slow, tight-binding histone deacetylase inhibitors with picomolar affinities

B Kitir, AR Maolanon, RG Ohm, AR Colaco… - Biochemistry, 2017 - ACS Publications
Histone deacetylases (HDACs) are validated targets for treatment of certain cancer types
and play numerous regulatory roles in biology, ranging from epigenetics to metabolism …