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Bromodomain inhibitors and therapeutic applications
Current Opinion in Chemical Biology, 2023 The bromodomain acts to recognize acetylated lysine in histones and transcription proteins and plays a fundamental role in chromatin-based cellular processes including gene transcription and chromatin remodeling.
Ming-Ming Zhou
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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 +2 more sources
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
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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
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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
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Frontiers in Endocrinology, 2022 Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D).
Joshua A. Nord +8 more
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Cell Reports, 2017 Summary BET inhibitors (BETi) target bromodomain-containing proteins and are currently being evaluated as anti-cancer agents. We find that maximal therapeutic effects of BETi in a Myc-driven B cell lymphoma model required an intact host immune system ...
Simon J Hogg +2 more
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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
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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
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Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies.
Cancer Cell, 2023 CCS1477 (inobrodib) is a potent, selective EP300/CBP bromodomain inhibitor which induces cell-cycle arrest and differentiation in hematologic malignancy model systems.
L. Nicosia +22 more
semanticscholar +1 more source