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 …
transcriptional regulators required for efficient expression of several growth promoting and …
BET bromodomain inhibitors: novel design strategies and therapeutic applications
The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists
of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer …
of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer …
Discovery of tetrahydroquinoxalines as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the second bromodomain
RP Law, SJ Atkinson, P Bamborough… - Journal of Medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine
residues on histone proteins. The four BET bromodomains—BRD2, BRD3, BRD4, and …
residues on histone proteins. The four BET bromodomains—BRD2, BRD3, BRD4, and …
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 …
bromodomain and extra‐terminal (BET) family, is a chromatin reader protein interpreting …
AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies
The bromodomain and extraterminal (BET) protein BRD4 regulates gene expression via
recruitment of transcriptional regulatory complexes to acetylated chromatin …
recruitment of transcriptional regulatory complexes to acetylated chromatin …
The bromodomain and extra-terminal domain (BET) family: functional anatomy of BET paralogous proteins
Y Taniguchi - International journal of molecular sciences, 2016 - mdpi.com
The Bromodomain and Extra-Terminal Domain (BET) family of proteins is characterized by
the presence of two tandem bromodomains and an extra-terminal domain. The mammalian …
the presence of two tandem bromodomains and an extra-terminal domain. The mammalian …
[HTML][HTML] Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery
As a conserved protein interaction module that recognizes and binds to acetylated lysine,
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
Discovery and characterization of small molecule inhibitors of the BET family bromodomains
C Chung, H Coste, JH White, O Mirguet… - Journal of medicinal …, 2011 - ACS Publications
Epigenetic mechanisms of gene regulation have a profound role in normal development and
disease processes. An integral part of this mechanism occurs through lysine acetylation of …
disease processes. An integral part of this mechanism occurs through lysine acetylation of …
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 …
and plays a fundamental role in chromatin-based cellular processes including gene …
The mechanisms behind the therapeutic activity of BET bromodomain inhibition
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …