Emerging roles of and therapeutic strategies targeting BRD4 in cancer

ME White, JM Fenger, WE Carson III - Cellular immunology, 2019 - Elsevier
Abstract The Bromodomain and Extra-terminal (BET) family of proteins were first recognized
as important epigenetic regulators in inflammatory processes; however, there is increasing …

Analysis and interpretation of the impact of missense variants in cancer

M Petrosino, L Novak, A Pasquo, R Chiaraluce… - International Journal of …, 2021 - mdpi.com
Large scale genome sequencing allowed the identification of a massive number of genetic
variations, whose impact on human health is still unknown. In this review we analyze, by an …

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 …

Reading cancer: chromatin readers as druggable targets for cancer treatment

C Mio, S Bulotta, D Russo, G Damante - Cancers, 2019 - mdpi.com
The epigenetic machinery deputed to control histone post-translational modifications is
frequently dysregulated in cancer cells. With epigenetics being naturally reversible, it …

Discovery of a hidden transient state in all bromodomain families

L Raich, K Meier, J Günther, CD Christ… - Proceedings of the …, 2021 - National Acad Sciences
Bromodomains (BDs) are small protein modules that interact with acetylated marks in
histones. These posttranslational modifications are pivotal to regulate gene expression …

Targeting the epigenetic reader “BET” as a therapeutic strategy for cancer

A Wahi, N Manchanda, P Jain, HR Jadhav - Bioorganic Chemistry, 2023 - Elsevier
Bromodomain and extraterminal (BET) proteins have the ability to bind to acetylated lysine
residues present in both histones and non-histone proteins. This binding is facilitated by the …

Bromodomain interactions with acetylated histone 4 peptides in the BRD4 tandem domain: effects on domain dynamics and internal flexibility

S Wernersson, R Bobby, L Flavell, AG Milbradt… - Biochemistry, 2022 - ACS Publications
The bromodomain and extra-terminal (BET) protein BRD4 regulates gene expression via
recruitment of transcriptional regulatory complexes to acetylated chromatin. Like other BET …

Biochemical and cellular insights into the Baz2B protein, a non-catalytic subunit of the chromatin remodeling complex

M Breindl, D Spitzer, R Gerasimaitė… - Nucleic Acids …, 2024 - academic.oup.com
Baz2B is a regulatory subunit of the ATP-dependent chromatin remodeling complexes BRF1
and BRF5, which control access to DNA during DNA-templated processes. Baz2B has been …

[HTML][HTML] Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma—An aggressive and fatal disease

A Stirnweiss, J Oommen, RS Kotecha, UR Kees… - Oncotarget, 2017 - ncbi.nlm.nih.gov
NUT midline carcinoma (NMC) is a rare and aggressive cancer, with survival typically less
than seven months, that can arise in people of any age. Genetically, NMC is defined by the …

The phosphoglycerate kinase 1 variants found in carcinoma cells display different catalytic activity and conformational stability compared to the native enzyme

A Fiorillo, M Petrosino, A Ilari, A Pasquo, A Cipollone… - PLoS …, 2018 - journals.plos.org
Cancer cells are able to survive in difficult conditions, reprogramming their metabolism
according to their requirements. Under hypoxic conditions they shift from oxidative …