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 …

Regulation of Nuclear Factor-KappaB (NF-κB) signaling pathway by non-coding RNAs in cancer: Inhibiting or promoting carcinogenesis?

S Mirzaei, A Zarrabi, F Hashemi, A Zabolian, H Saleki… - Cancer Letters, 2021 - Elsevier
The nuclear factor-kappaB (NF-κB) signaling pathway is considered as a potential
therapeutic target in cancer therapy. It has been well established that transcription factor NF …

Targeting transcription cycles in cancer

SJ Vervoort, JR Devlin, N Kwiatkowski, M Teng… - Nature Reviews …, 2022 - nature.com
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …

Bromodomain biology and drug discovery

N Zaware, MM Zhou - Nature structural & molecular biology, 2019 - nature.com
The bromodomain (BrD) is a conserved structural module found in chromatin-and
transcription-associated proteins that acts as the primary reader for acetylated lysine …

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 …

Targeted degradation of the enhancer lysine acetyltransferases CBP and p300

R Vannam, J Sayilgan, S Ojeda, B Karakyriakou… - Cell chemical …, 2021 - cell.com
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 …

Histone-deacetylase inhibitors: novel drugs for the treatment of cancer

RW Johnstone - Nature reviews Drug discovery, 2002 - nature.com
The opposing actions of histone acetyltransferases (HATs) and histone deacetylases
(HDACs) allow gene expression to be exquisitely regulated through chromatin remodelling …

Bromodomains as therapeutic targets

S Muller, P Filippakopoulos, S Knapp - Expert reviews in molecular …, 2011 - cambridge.org
Acetylation of lysine residues is a post-translational modification with broad relevance to
cellular signalling and disease biology. Enzymes that 'write'(histone acetyltransferases …

Histone deacetylase inhibitors: overview and perspectives

M Dokmanovic, C Clarke, PA Marks - Molecular cancer research, 2007 - AACR
Histone deacetylase inhibitors (HDACi) comprise structurally diverse compounds that are a
group of targeted anticancer agents. The first of these new HDACi, vorinostat …

Aberrant epigenetic landscape in cancer: how cellular identity goes awry

M Berdasco, M Esteller - Developmental cell, 2010 - cell.com
Appropriate patterns of DNA methylation and histone modifications are required to assure
cell identity, and their deregulation can contribute to human diseases, such as cancer. Our …