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 …

[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 …

Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone …

K Balasubramanyam, RA Varier, M Altaf… - Journal of Biological …, 2004 - ASBMB
Acetylation of histones and non-histone proteins is an important post-translational
modification involved in the regulation of gene expression in eukaryotes and all viral DNA …

Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor

EM Bowers, G Yan, C Mukherjee, A Orry, L Wang… - Chemistry & biology, 2010 - cell.com
The histone acetyltransferase (HAT) p300/CBP is a transcriptional coactivator implicated in
many gene regulatory pathways and protein acetylation events. Although p300 inhibitors …

Acetylation of non-histone proteins modulates cellular signalling at multiple levels

S Spange, T Wagner, T Heinzel, OH Krämer - The international journal of …, 2009 - Elsevier
This review focuses on the posttranslational acetylation of non-histone proteins, which
determines vital regulatory processes. The recruitment of histone acetyltransferases and …

Bromodomain inhibitors and cancer therapy: From structures to applications

M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …

Cancer chemoprevention by dietary polyphenols: promising role for epigenetics

A Link, F Balaguer, A Goel - Biochemical pharmacology, 2010 - Elsevier
Epigenetics refers to heritable changes that are not encoded in the DNA sequence itself, but
play an important role in the control of gene expression. In mammals, epigenetic …

Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression

K Balasubramanyam, M Altaf, RA Varier… - Journal of Biological …, 2004 - ASBMB
Histone acetylation is a diagnostic feature of transcriptionally active genes. The proper
recruitment and function of histone acetyltransferases (HATs) and deacetylases (HDACs) …

Use of epigenetic drugs in disease: an overview

S Heerboth, K Lapinska, N Snyder… - Genetics & …, 2014 - journals.sagepub.com
Epigenetic changes such as DNA methylation and histone methylation and acetylation alter
gene expression at the level of transcription by upregulating, downregulating, or silencing …