The Roles of Histone Deacetylases and Their Inhibitors in Cancer Therapy
Frontiers in Cell and Developmental Biology, 2020 Genetic mutations and abnormal gene regulation are key mechanisms underlying tumorigenesis. Nucleosomes, which consist of DNA wrapped around histone cores, represent the basic units of chromatin. The fifth amino group (Nε) of histone lysine residues is a
Guo Li +4 more
doaj +2 more sources
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth [PDF]
Nature, 2018 Acetylation of histones by lysine acetyltransferases (KATs) is essential for chromatin organization and function1. Among the genes coding for the MYST family of KATs (KAT5–KAT8) are the oncogenes KAT6A (also known as MOZ) and KAT6B (also known as MORF ...
J. Baell +51 more
semanticscholar +2 more sources
Metformin Induces Apoptosis in Human Pancreatic Cancer (PC) Cells Accompanied by Changes in the Levels of Histone Acetyltransferases (Particularly, p300/CBP-Associated Factor (PCAF) Protein Levels). [PDF]
Pharmaceuticals (Basel), 2023 Szymczak-Pajor I +7 more
europepmc +2 more sources
Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases [PDF]
Drug Discovery Today, 2011 Lysine acetylation is a reversible post-translational modification (PTM) of cellular proteins and represents an important regulatory switch in signal transduction.
F. Dekker +2 more
semanticscholar +2 more sources
Histone Acetyltransferases in Smooth Muscle Cell Phenotype Switching: Redundant No Longer. [PDF]
Circulation, 2022 Jaffe IZ.
europepmc +2 more sources
Posttranslational regulation of the GCN5 and PCAF acetyltransferases
PLoS Genetics, 2022 General control nonderepressible 5 protein (Gcn5) and its homologs, including p300/CBP-associated factor (PCAF), are lysine acetyltransferases that modify both histone and non-histone proteins using acetyl coenzyme A as a donor substrate.
Onyekachi E. Ononye, Michael Downey
doaj +2 more sources
Roles of histone acetylation sites in cardiac hypertrophy and heart failure
Frontiers in Cardiovascular Medicine, 2023 Heart failure results from various physiological and pathological stimuli that lead to cardiac hypertrophy. This pathological process is common in several cardiovascular diseases and ultimately leads to heart failure.
Masafumi Funamoto +3 more
doaj +1 more source
Amide-derived lysine analogues as substrates and inhibitors of histone lysine methyltransferases and acetyltransferases [PDF]
, 2022 Histone lysine methyltransferases and acetyltransferases are two classes of epigenetic enzymes that play pivotal roles in human gene regulation. Although they both recognise and posttranslationally modify lysine residues in histone proteins, their ...
Boltje, Thomas J. +6 more
core +1 more source
Transcription shapes genome-wide histone acetylation patterns
Nature Communications, 2021 Histone acetylation is a ubiquitous hallmark of transcription. Here the authors provide evidence that the majority of histone acetylation is dependent on transcription, specifically due to the requirement of RNAPII for the recruitment and activity of ...
Benjamin J. E. Martin +6 more
doaj +1 more source