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 …

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 …

Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery

D Liang, Y Yu, Z Ma - European journal of medicinal chemistry, 2020 - Elsevier
As epigenetic readers of the histone code, BRD4 is the most extensively and thoroughly
studied member of BET family, which plays a critical role in many human diseases including …

Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains

G Zhang, AN Plotnikov, E Rusinova… - Journal of medicinal …, 2013 - ACS Publications
BRD4, characterized by two acetyl-lysine binding bromodomains and an extra-terminal (ET)
domain, is a key chromatin organizer that directs gene activation in chromatin through …

A patent review of BRD4 inhibitors (2013-2019)

T Lu, W Lu, C Luo - Expert Opinion on Therapeutic Patents, 2020 - Taylor & Francis
Introduction: The bromodomain-containing protein 4 (BRD4), a member of the bromodomain
and extra-terminal (BET) family, functions as an 'epigenetic reader'that binds to acetylated …

Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

Dual‐target inhibitors of bromodomain and extra‐terminal proteins in cancer: A review from medicinal chemistry perspectives

L Feng, G Wang, Y Chen, G He, B Liu… - Medicinal research …, 2022 - Wiley Online Library
Abstract Bromodomain‐containing protein 4 (BRD4), as the most studied member of the
bromodomain and extra‐terminal (BET) family, is a chromatin reader protein interpreting …

[HTML][HTML] Post-translational modifications of BRD4: therapeutic targets for tumor

N Liu, R Ling, X Tang, Y Yu, Y Zhou, D Chen - Frontiers in oncology, 2022 - frontiersin.org
Bromodomain-containing protein 4 (BRD4), a member of the bromodomain and
extraterminal (BET) family, is considered to be a major driver of cancer cell growth and a …

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 …

[HTML][HTML] 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 …