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 …

Histone deacetylases: a saga of perturbed acetylation homeostasis in cancer

S Parbin, S Kar, A Shilpi, D Sengupta… - … of Histochemistry & …, 2014 - journals.sagepub.com
In the current era of genomic medicine, diseases are identified as manifestations of
anomalous patterns of gene expression. Cancer is the principal example among such …

Chemically induced degradation of sirtuin 2 (Sirt2) by a proteolysis targeting chimera (PROTAC) based on sirtuin rearranging ligands (SirReals)

M Schiedel, D Herp, S Hammelmann… - Journal of medicinal …, 2018 - ACS Publications
Here we report the development of a proteolysis targeting chimera (PROTAC) based on the
combination of the unique features of the sirtuin rearranging ligands (SirReals) as highly …

Selective Sirt2 inhibition by ligand-induced rearrangement of the active site

T Rumpf, M Schiedel, B Karaman, C Roessler… - Nature …, 2015 - nature.com
Sirtuins are a highly conserved class of NAD+-dependent lysine deacylases. The human
isotype Sirt2 has been implicated in the pathogenesis of cancer, inflammation and …

Development of first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools for dual inhibition of tubulin deacetylation

L Sinatra, A Vogelmann, F Friedrich… - Journal of medicinal …, 2023 - ACS Publications
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6
(HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration …

Synthesis and biological investigation of phenothiazine-based benzhydroxamic acids as selective histone deacetylase 6 inhibitors

K Vögerl, N Ong, J Senger, D Herp… - Journal of medicinal …, 2019 - ACS Publications
The phenothiazine system was identified as a favorable cap group for potent and selective
histone deacetylase 6 (HDAC6) inhibitors. Here, we report the preparation and systematic …

Structure–Activity Studies on Suramin Analogues as Inhibitors of NAD+‐Dependent Histone Deacetylases (Sirtuins)

J Trapp, R Meier, D Hongwiset… - ChemMedChem …, 2007 - Wiley Online Library
Suramin is a symmetric polyanionic naphthylurea originally used for the treatment of
trypanosomiasis and onchocerciasis. Suramin and diverse analogues exhibit a broad range …

Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects In Vitro and Neuroprotective Effects in a …

F He, CJ Chou, M Scheiner, E Poeta… - Journal of medicinal …, 2021 - ACS Publications
The structures of melatonin and ferulic acid were merged into tertiary amide-based histone
deacetylase 6 (HDAC6) inhibitors to develop multi-target-directed inhibitors for …

Harnessing the role of HDAC6 in idiopathic pulmonary fibrosis: design, synthesis, structural analysis, and biological evaluation of potent inhibitors

G Campiani, C Cavella, JD Osko… - Journal of medicinal …, 2021 - ACS Publications
Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a
progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities …

Synthesis and biological investigation of oxazole hydroxamates as highly selective histone deacetylase 6 (HDAC6) inhibitors

J Senger, J Melesina, M Marek, C Romier… - Journal of medicinal …, 2016 - ACS Publications
Histone deacetylase 6 (HDAC6) catalyzes the removal of an acetyl group from lysine
residues of several non-histone proteins. Here we report the preparation of thiazole …