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 …

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 …

The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3

S Rahman, ME Sowa, M Ottinger, JA Smith… - … and cellular biology, 2011 - Taylor & Francis
Bromodomain protein 4 (Brd4) plays critical roles in development, cancer progression, and
virus-host pathogenesis. To gain mechanistic insight into the various biological functions of …

Retroviral DNA integration

P Lesbats, AN Engelman, P Cherepanov - Chemical reviews, 2016 - ACS Publications
The integration of a DNA copy of the viral RNA genome into host chromatin is the defining
step of retroviral replication. This enzymatic process is catalyzed by the virus-encoded …

Lysine acetylation and cancer: A proteomics perspective

J Gil, A Ramírez-Torres, S Encarnación-Guevara - Journal of proteomics, 2017 - Elsevier
Lysine acetylation is a reversible modification controlled by two groups of enzymes: lysine
acetyltransferases (KATs) and lysine deacetylases (KDACs). Acetylated lysine residues are …

Place your BETs: the therapeutic potential of bromodomains

RK Prinjha, J Witherington, K Lee - Trends in pharmacological sciences, 2012 - cell.com
Therapeutic targeting of the processes that regulate histone modification is a growing area
of scientific exploration. Although most interest has concentrated on the various families of …

BET proteins promote efficient murine leukemia virus integration at transcription start sites

A Sharma, RC Larue, MR Plumb… - Proceedings of the …, 2013 - National Acad Sciences
The selection of chromosomal targets for retroviral integration varies markedly, tracking with
the genus of the retrovirus, suggestive of targeting by binding to cellular factors. γ-Retroviral …

Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1

M Jung, M Philpott, S Müller, J Schulze… - Journal of biological …, 2014 - ASBMB
Bromodomain protein 4 (BRD4) is a member of the bromodomain and extra-terminal domain
(BET) protein family. It binds to acetylated histone tails via its tandem bromodomains BD1 …

BRD4 in physiology and pathology:''BET''on its partners

Y Liang, J Tian, T Wu - Bioessays, 2021 - Wiley Online Library
Abstract Bromodomain‐containing 4 (BRD4), a member of Bromo and Extra‐Terminal (BET)
family, recognizes acetylated histones and is of importance in transcription, replication, and …

Bromo-and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration

SS Gupta, T Maetzig, GN Maertens, A Sharif… - Journal of …, 2013 - Am Soc Microbiol
Retroviral integrase (IN) proteins catalyze the permanent integration of proviral genomes
into host DNA with the help of cellular cofactors. Lens epithelium-derived growth factor …