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 …
modifications that regulate gene activity beyond the underlying sequence. Epigenetic …
[HTML][HTML] Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents
Q Chen, B Yang, X Liu, XD Zhang, L Zhang, T Liu - Theranostics, 2022 - ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …
sequence homology and functional overlap and co-operation, are emerging as critical …
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
LM Lasko, CG Jakob, RP Edalji, W Qiu, D Montgomery… - Nature, 2017 - nature.com
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases
(HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of …
(HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of …
Lysine acetylation goes global: from epigenetics to metabolism and therapeutics
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
50 years of protein acetylation: from gene regulation to epigenetics, metabolism and beyond
Abstract In 1964, Vincent Allfrey and colleagues reported the identification of histone
acetylation and with deep insight proposed a regulatory role for this protein modification in …
acetylation and with deep insight proposed a regulatory role for this protein modification in …
Epigenetic protein families: a new frontier for drug discovery
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …
establishes normal cellular phenotypes but also contributes to human diseases. At the …
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300
The enhancer factors CREB-binding protein (CBP) and p300 (also known as KAT3A and
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …
Photoaffinity labeling in target-and binding-site identification
E Smith, I Collins - Future medicinal chemistry, 2015 - Taylor & Francis
Photoaffinity labeling (PAL) using a chemical probe to covalently bind its target in response
to activation by light has become a frequently used tool in drug discovery for identifying new …
to activation by light has become a frequently used tool in drug discovery for identifying new …
Histone acetyltransferases
▪ Abstract Transcriptional regulation in eukaryotes occurs within a chromatin setting and is
strongly influenced by nucleosomal barriers imposed by histone proteins. Among the well …
strongly influenced by nucleosomal barriers imposed by histone proteins. Among the well …