Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

Y Cheng, C He, M Wang, X Ma, F Mo, S Yang… - Signal transduction and …, 2019 - nature.com
Epigenetic alternations concern heritable yet reversible changes in histone or DNA
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …

Erasers of histone acetylation: the histone deacetylase enzymes

E Seto, M Yoshida - Cold Spring Harbor perspectives in …, 2014 - cshperspectives.cshlp.org
Histone deacetylases (HDACs) are enzymes that catalyze the removal of acetyl functional
groups from the lysine residues of both histone and nonhistone proteins. In humans, there …

Class I histone deacetylases (HDAC1–3) are histone lysine delactylases

C Moreno-Yruela, D Zhang, W Wei, M Bæk, W Liu… - Science …, 2022 - science.org
Lysine L-lactylation [K (L-la)] is a newly discovered histone mark stimulated under conditions
of high glycolysis, such as the Warburg effect. K (L-la) is associated with functions that are …

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 …

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 …

Microbiota-derived metabolite promotes HDAC3 activity in the gut

S Wu, S Hashimoto-Hill, V Woo, EM Eshleman, J Whitt… - Nature, 2020 - nature.com
The coevolution of mammalian hosts and their beneficial commensal microbes has led to
development of symbiotic host–microbiota relationships. Epigenetic machinery permits …

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 …

Lysine acetylation goes global: from epigenetics to metabolism and therapeutics

I Ali, RJ Conrad, E Verdin, M Ott - Chemical reviews, 2018 - ACS Publications
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Diverse modes of H3K36me3-guided nucleosomal deacetylation by Rpd3S

H Guan, P Wang, P Zhang, C Ruan, Y Ou, B Peng… - Nature, 2023 - nature.com
Context-dependent dynamic histone modifications constitute a key epigenetic mechanism in
gene regulation,,–. The Rpd3 small (Rpd3S) complex recognizes histone H3 trimethylation …