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 …

[HTML][HTML] BET inhibitors: a novel epigenetic approach

DB Doroshow, JP Eder, PM LoRusso - Annals of Oncology, 2017 - Elsevier
Epigenetics has been defined as 'the structural adaptation of chromosomal regions so as to
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …

Selective inhibition of BET bromodomains

P Filippakopoulos, J Qi, S Picaud, Y Shen, WB Smith… - Nature, 2010 - nature.com
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts
have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and …

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

BN Devaiah, C Case-Borden, A Gegonne… - Nature structural & …, 2016 - nature.com
Abstract Bromodomain protein 4 (BRD4) is a chromatin-binding protein implicated in cancer
and autoimmune diseases that functions as a scaffold for transcription factors at promoters …

BET domain co-regulators in obesity, inflammation and cancer

AC Belkina, GV Denis - Nature reviews Cancer, 2012 - nature.com
The bromodomain is a highly conserved motif of 110 amino acids that is bundled into four
anti-parallel α-helices and found in proteins that interact with chromatin, such as …

Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

S Picaud, C Wells, I Felletar… - Proceedings of the …, 2013 - National Acad Sciences
Bromodomains have emerged as attractive candidates for the development of inhibitors
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …

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 …

[HTML][HTML] Control of embryonic stem cell identity by BRD4-dependent transcriptional elongation of super-enhancer-associated pluripotency genes

R Di Micco, B Fontanals-Cirera, V Low, P Ntziachristos… - Cell reports, 2014 - cell.com
Transcription factors and chromatin-remodeling complexes are key determinants of
embryonic stem cell (ESC) identity. Here, we demonstrate that BRD4, a member of the …

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

S Picaud, D Da Costa, A Thanasopoulou… - Cancer research, 2013 - AACR
Bromo and extra terminal (BET) proteins (BRD2, BRD3, BRD4, and BRDT) are
transcriptional regulators required for efficient expression of several growth promoting and …