BRD4 and Cancer: going beyond transcriptional regulation

B Donati, E Lorenzini, A Ciarrocchi - Molecular cancer, 2018 - Springer
BRD4, member of the Bromodomain and Extraterminal (BET) protein family, is largely
acknowledged in cancer for its role in super-enhancers (SEs) organization and oncogenes …

Metabolic regulation of gene expression through histone acylations

BR Sabari, D Zhang, CD Allis, Y Zhao - Nature reviews Molecular cell …, 2017 - nature.com
Eight types of short-chain Lys acylations have recently been identified on histones:
propionylation, butyrylation, 2-hydroxyisobutyrylation, succinylation, malonylation …

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung… - Science, 2020 - science.org
The two tandem bromodomains of the BET (bromodomain and extraterminal domain)
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …

Time-resolved analysis reveals rapid dynamics and broad scope of the CBP/p300 acetylome

BT Weinert, T Narita, S Satpathy, B Srinivasan… - Cell, 2018 - cell.com
The acetyltransferases CBP and p300 are multifunctional transcriptional co-activators. Here,
we combined quantitative proteomics with CBP/p300-specific catalytic inhibitors …

The BET family in immunity and disease

N Wang, R Wu, D Tang, R Kang - Signal transduction and targeted …, 2021 - nature.com
Innate immunity serves as the rapid and first-line defense against invading pathogens, and
this process can be regulated at various levels, including epigenetic mechanisms. The …

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer

T Fujisawa, P Filippakopoulos - Nature reviews Molecular cell biology, 2017 - nature.com
Bromodomains (BRDs) are evolutionarily conserved protein–protein interaction modules
that are found in a wide range of proteins with diverse catalytic and scaffolding functions and …

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 …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …

The mechanisms behind the therapeutic activity of BET bromodomain inhibition

J Shi, CR Vakoc - Molecular cell, 2014 - cell.com
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …

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 …