The timeline of epigenetic drug discovery: from reality to dreams
The flexibility of the epigenome has generated an enticing argument to explore its reversion
through pharmacological treatments as a strategy to ameliorate disease phenotypes. All …
through pharmacological treatments as a strategy to ameliorate disease phenotypes. All …
The functions of BET proteins in gene transcription of biology and diseases
KL Cheung, C Kim, MM Zhou - Frontiers in molecular biosciences, 2021 - frontiersin.org
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2,
BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional …
BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional …
Stromal induction of BRD4 phosphorylation results in chromatin remodeling and BET inhibitor resistance in colorectal cancer
W Wang, YA Tang, Q Xiao, WC Lee, B Cheng… - Nature …, 2021 - nature.com
BRD4, a Bromodomain and Extraterminal (BET) protein family member, is a promising anti-
cancer drug target. However, resistance to BET inhibitors targeting BRD4 is common in solid …
cancer drug target. However, resistance to BET inhibitors targeting BRD4 is common in solid …
Targeting bromodomain and extraterminal proteins for drug discovery: from current progress to technological development
P Tang, J Zhang, J Liu, CM Chiang… - Journal of medicinal …, 2021 - ACS Publications
Bromodomain and extraterminal (BET) proteins bind acetylated lysine residues in histones
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …
In silico molecular docking studies and MM/GBSA analysis of coumarin-carbonodithioate hybrid derivatives divulge the anticancer potential against breast cancer
SV Pattar, SA Adhoni, CM Kamanavalli… - Beni-Suef University …, 2020 - Springer
Background There are many biomarkers associated with breast cancer. Higher expression
of PIK3CA (Phosphoinositide 3-kinase Cα), in its upregulated form, is associated with Hr+ …
of PIK3CA (Phosphoinositide 3-kinase Cα), in its upregulated form, is associated with Hr+ …
Structural mechanism of BRD4-NUT and p300 bipartite interaction in propagating aberrant gene transcription in chromatin in NUT carcinoma
D Yu, Y Liang, C Kim, A Jaganathan, D Ji… - Nature …, 2023 - nature.com
BRD4-NUT, a driver fusion mutant in rare and highly aggressive NUT carcinoma, acts in
aberrant transcription of anti-differentiation genes by recruiting histone acetyltransferase …
aberrant transcription of anti-differentiation genes by recruiting histone acetyltransferase …
BET proteins: Biological functions and therapeutic interventions
J Guo, Q Zheng, Y Peng - Pharmacology & Therapeutics, 2023 - Elsevier
Bromodomain and extra-terminal (BET) family member proteins (BRD2, BRD3, BRD4 and
BRDT) play a pivotal role in interpreting the epigenetic information of histone Kac …
BRDT) play a pivotal role in interpreting the epigenetic information of histone Kac …
Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors
O Bechter, P Schöffski - Pharmacology & therapeutics, 2020 - Elsevier
Bromodomains are protein-protein interaction modules with a great diversity in terms of
number of proteins and their function. The bromodomain and extraterminal protein (BET) …
number of proteins and their function. The bromodomain and extraterminal protein (BET) …
Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy
ZQ Wang, ZC Zhang, YY Wu, YN Pi, SH Lou… - Signal transduction and …, 2023 - nature.com
BET proteins, which influence gene expression and contribute to the development of cancer,
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …
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 …
family, recognizes acetylated histones and is of importance in transcription, replication, and …