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 …
Histone deacetylases: a saga of perturbed acetylation homeostasis in cancer
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 …
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 …
combination of the unique features of the sirtuin rearranging ligands (SirReals) as highly …
Selective Sirt2 inhibition by ligand-induced rearrangement of the active site
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 …
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 …
(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 …
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 …
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 …
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 …
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 …
residues of several non-histone proteins. Here we report the preparation of thiazole …