Bromodomain Proteins in HIV Infection [PDF]
Viruses, 2013 Bromodomains are conserved protein modules of ~110 amino acids that bind acetylated lysine residues in histone and non-histone proteins. Bromodomains are present in many chromatin-associated transcriptional regulators and have been linked to diverse ...
Melanie Ott +2 more
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Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains [PDF]
Journal of Medicinal Chemistry, 2020 Non-BET bromodomain-containing proteins have become attractive targets for the development of novel therapeutics targeting epigenetic pathways. To help facilitate the target validation of this class of proteins, structurally diverse small-molecule ligands and methodologies to produce selective inhibitors in a predictable fashion are in high demand ...
Michael A. Clegg +17 more
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Bromodomain and extra-terminal domain (BET) proteins regulate melanocyte differentiation
Epigenetics & Chromatin, 2020 Background Pharmacologic inhibition of bromodomain and extra-terminal (BET) proteins is currently being explored as a new therapeutic approach in cancer.
Archit Trivedi +9 more
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Bromodomain dimers: A case study of BRD4 and family-wide AlphaFold predictions [PDF]
Structural DynamicsBromodomains are conserved acetyl-lysine reader domains that play a central role in the assembly of transcriptional regulatory complexes. While generally presumed to function as monomers, bromodomain homo-dimers have been identified, and several ...
Alisa S. Dengler +3 more
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Functions of bromodomain-containing proteins and their roles in homeostasis and cancer [PDF]
Nature Reviews Molecular Cell Biology, 2017 Bromodomains (BRDs) are evolutionarily conserved protein-protein interaction modules that are found in a wide range of proteins with diverse catalytic and scaffolding functions and are present in most tissues. BRDs selectively recognize and bind to acetylated Lys residues - particularly in histones - and thereby have important roles in the regulation ...
Panagis Filippakopoulos
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Spotlight on Plant Bromodomain Proteins
Biology, 2023 Bromodomain-containing proteins (BRD-proteins) are the “readers” of histone lysine acetylation, translating chromatin state into gene expression.
Eirini Bardani +4 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 Minireview on BET Inhibitors: Beyond Bromodomain Targeting
BiomedicinesBromodomain and extra-terminal domain (BET) proteins are epigenetic readers that recognize the histone acetylation code and play a critical role in regulating gene transcription.
Mikhail S. Iudin +4 more
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Novel Benzoisoxazoloazepine Inhibitors of Bromodomain-Containing Proteins. [PDF]
ACS Med Chem Lett, 2014 Rosse G.
europepmc +4 more sources
Applying ⁸⁹Zr-Transferrin To Study the Pharmacology of Inhibitors to BET Bromodomain Containing Proteins. [PDF]
Mol Pharm, 2016 Chromatin modifying proteins are attractive drug targets in oncology, given the fundamental reliance of cancer on altered transcriptional activity. Multiple transcription factors can be impacted downstream of primary target inhibition, thus making it ...
Doran MG +8 more
europepmc +2 more sources