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 …
Recent developments of HDAC inhibitors: Emerging indications and novel molecules
AD Bondarev, MM Attwood, J Jonsson… - British journal of …, 2021 - Wiley Online Library
The histone deacetylase (HDAC) enzymes, a class of epigenetic regulators, are historically
well established as attractive therapeutic targets. During investigation of trends within …
well established as attractive therapeutic targets. During investigation of trends within …
[HTML][HTML] The roles of histone deacetylases and their inhibitors in cancer therapy
G Li, Y Tian, WG Zhu - Frontiers in cell and developmental biology, 2020 - frontiersin.org
Genetic mutations and abnormal gene regulation are key mechanisms underlying
tumorigenesis. Nucleosomes, which consist of DNA wrapped around histone cores …
tumorigenesis. Nucleosomes, which consist of DNA wrapped around histone cores …
[HTML][HTML] A short guide to histone deacetylases including recent progress on class II enzymes
SY Park, JS Kim - Experimental & molecular medicine, 2020 - nature.com
The interaction between histones and DNA is important for eukaryotic gene expression. A
loose interaction caused, for example, by the neutralization of a positive charge on the …
loose interaction caused, for example, by the neutralization of a positive charge on the …
Spermidine in health and disease
BACKGROUND As the world population ages, chronic diseases such as diabetes,
cardiovascular disease, cancer, and neurodegeneration become ever more prevalent …
cardiovascular disease, cancer, and neurodegeneration become ever more prevalent …
[HTML][HTML] Therapeutic targets for cardiac fibrosis: from old school to next-gen
Cardiovascular diseases remain the leading cause of death worldwide, with pathological
fibrotic remodeling mediated by activated cardiac myofibroblasts representing a unifying …
fibrotic remodeling mediated by activated cardiac myofibroblasts representing a unifying …
[HTML][HTML] Mechanisms of spermidine-induced autophagy and geroprotection
Aging involves the systemic deterioration of all known cell types in most eukaryotes. Several
recently discovered compounds that extend the healthspan and lifespan of model organisms …
recently discovered compounds that extend the healthspan and lifespan of model organisms …
[HTML][HTML] Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability
G Milazzo, D Mercatelli, G Di Muzio, L Triboli… - Genes, 2020 - mdpi.com
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …
removing acetyl groups from histones and other protein regulatory factors, with functional …
[HTML][HTML] Anticancer therapy with HDAC inhibitors: mechanism-based combination strategies and future perspectives
R Jenke, N Reßing, FK Hansen, A Aigner, T Büch - Cancers, 2021 - mdpi.com
Simple Summary Beyond mutations, epigenetic changes have been described as drivers for
cancer as well. While leaving the overall DNA structure intact, they can be responsible for …
cancer as well. While leaving the overall DNA structure intact, they can be responsible for …
Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target
S Lechner, MIP Malgapo, C Grätz… - Nature chemical …, 2022 - nature.com
Drugs that target histone deacetylase (HDAC) entered the pharmacopoeia in the 2000s.
However, some enigmatic phenotypes suggest off-target engagement. Here, we developed …
However, some enigmatic phenotypes suggest off-target engagement. Here, we developed …