Recent Progress and Prospect in Studying Selective Inhibitors Toward Bromodomain Family Members [PDF]
MoleculesBromodomain (BRD)-containing proteins are gaining attention as key targets in epigenetic drug development. BRDs bind to acetylated lysine residues on histones and other proteins, significantly impacting transcriptional regulation and chromatin remodeling.
Jianzhong Chen +3 more
doaj +2 more sources
Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]
PLoS ONE, 2016 Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori +7 more
doaj +4 more sources
High affinity binding of H3K14ac through collaboration of bromodomains 2, 4 and 5 is critical for the molecular and tumor suppressor functions of PBRM1 [PDF]
Molecular Oncology, 2019 Polybromo‐1 (PBRM1) is an important tumor suppressor in kidney cancer. It contains six tandem bromodomains (BDs), which are specialized structures that recognize acetyl‐lysine residues.
Lili Liao +10 more
doaj +3 more sources
A 5-Br-1-Propylisatin Derivative as a Promising BRD9 Ligand: Insights from Computational and STD NMR Investigation [PDF]
MoleculesBromodomain-containing protein 9 (BRD9) belongs to the non-canonical BAF chromatin remodeling complex and represents a relevant therapeutic target in pathologies featuring dysregulated epigenetic control.
Erica Gazzillo +5 more
doaj +2 more sources
eLife, 2021 Human bromodomain and extra-terminal domain (BET) family members are promising targets for therapy of cancer and immunoinflammatory diseases, but their mechanisms of action and functional redundancies are poorly understood.
Rafal Donczew, Steven Hahn
doaj +1 more source
Exploration of Targeted Anti-tumor Therapy, 2021 Aim: Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that play a fundamental role in transcription regulation. Preclinical and early clinical evidence sustain BET targeting as an anti-cancer approach.
Chiara Tarantelli +14 more
doaj +1 more source
BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications
Molecules, 2023 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-related and immunity-associated genes.
Kenneth K. W. To +3 more
doaj +1 more source
The Aggregation of ATAD2 Bromodomain in Solution
Chinese Journal of Magnetic Resonance, 2023 ATPase family AAA domain-containing protein 2 (ATAD2) is a chromatin regulator, also known as an oncogenic transcription cofactor. Its abnormal expression is closely related to the occurrence and development of various malignant tumors. ATAD2 consists of
WANG Yuanfang +5 more
doaj +1 more source
A Nutrient-Based Cellular Model to Characterize Acetylation-Dependent Protein-Protein Interactions
Frontiers in Molecular Biosciences, 2022 Cellular homeostasis requires the orderly expression of thousands of transcripts. Gene expression is regulated by numerous proteins that recognize post-translational modifications—in particular, the acetylation of lysine residues (Kac) on histones.
Jérémy Loehr +15 more
doaj +1 more source
The Functions of BET Proteins in Gene Transcription of Biology and Diseases
Frontiers in Molecular Biosciences, 2021 The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional regulators in biology.
Ka Lung Cheung +2 more
doaj +1 more source