Stabilizing Plasmodium falciparum proteins for small molecule drug discovery. [PDF]
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From Epigenetic Regulation to Protein Degradation: Emerging Strategies for Anti-Infective Drug Discovery. [PDF]
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Perturbation of BRD4 and p300 activity suppresses super enhancer‑driven <i>KLF6</i> expression in renal carcinoma. [PDF]
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Histone modification cross-talk: analytical tools and molecular mechanisms. [PDF]
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Functional Roles of Bromodomain Proteins in Cancer
Histone acetylation is generally associated with an open chromatin configuration that facilitates many cellular processes including gene transcription, DNA repair, and DNA replication. Aberrant levels of histone lysine acetylation are associated with the
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Privileged Scaffolds Targeting Bromodomain-containing Protein 4
Current Topics in Medicinal Chemistry, 2022Abstract: In recent years, bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra terminal domain (BET) family, has been one of the most widely studied targets. BRD4 is a transcriptional regulation factor, which regulates cell transcription, marks mammalian biological mitosis, regulates cell cycle, and plays an important role ...
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Research Progress of Selective Small Molecule Bromodomain-Containing Protein 9 Inhibitors
The bromodomain proteins, known as the key targets in epigenetics, are ‘readers’ of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling ...
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Bromodomain-Containing Protein 4: A Druggable Target
Current Drug Targets, 2019Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extraterminal family. BRD4 inhibitors can regulate acetylated lysine and form protein complexes that initiate transcriptional programs as an epigenetic regulator of the histone code. BRD4 was initially considered to be one of the most promising targets for combating malignant tumors.
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Acetyllysine-binding and function of bromodomain-containing proteins in chromatin
Frontiers in Bioscience, 2001Acetylated histones are generally associated with active chromatin. The bromodomain has recently been identified as a protein module capable of binding to acetylated lysine residues, and hence is able to mediate the recruitment of factors to acetylated chromatin. Functional studies of bromodomain-containing proteins indicate how this domain contributes
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