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   Articles with "bromodomain" as a keyword



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Yeast Bromodomain Factor 1 and Its Human Homolog TAF1 Play Conserved Roles in Promoting Homologous Recombination

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recommendations! Published in 2021 at "Advanced Science"

DOI: 10.1002/advs.202100753

Abstract: Abstract Histone acetylation is a key histone post‐translational modification that shapes chromatin structure, dynamics, and function. Bromodomain (BRD) proteins, the readers of acetyl‐lysines, are located in the center of the histone acetylation‐signaling network. How they… read more here.

Keywords: bromodomain factor; taf1; yeast bromodomain; bromodomain ... See more keywords
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Covalent Modification of Bromodomain Proteins by Peptides Containing a DNA Damage‐Induced, Histone Post‐Translational Modification

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recommendations! Published in 2022 at "ChemBioChem"

DOI: 10.1002/cbic.202200373

Abstract: An electrophilic 5‐methylene‐2‐pyrrolone modification (KMP) is produced at lysine residues of histone proteins in nucleosome core particles upon reaction with a commonly formed DNA lesion (C4‐AP). The nonenzymatic KMP modification is also generated in the… read more here.

Keywords: modification; histone; kmp; bromodomain ... See more keywords
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CG13250, a novel bromodomain inhibitor, suppresses proliferation of multiple myeloma cells in an orthotopic mouse model.

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recommendations! Published in 2017 at "Biochemical and biophysical research communications"

DOI: 10.1016/j.bbrc.2017.01.088

Abstract: Multiple myeloma (MM) is characterized by the clonal proliferation of neoplastic plasma cells. Despite a stream of new molecular targets based on better understanding of the disease, MM remains incurable. Epigenomic abnormalities contribute to the… read more here.

Keywords: inhibitor; cg13250; proliferation; multiple myeloma ... See more keywords
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Design, synthesis, and biological evaluation of tetrahydroquinolin derivatives as potent inhibitors of CBP bromodomain.

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recommendations! Published in 2020 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2020.103991

Abstract: CREB-binding protein (CBP) is a large multi-domain protein containing a HAT domain catalyzing transacetylation and a bromodomain responsible for acetylated lysine recognition. CBPs could act as transcription co-activators to regulate gene expression and have been… read more here.

Keywords: design synthesis; cbp bromodomain; cpin711 showed; cpin7 ... See more keywords
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Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.

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recommendations! Published in 2019 at "Cell reports"

DOI: 10.1016/j.celrep.2019.03.008

Abstract: Myeloid-derived suppressor cells (MDSCs) are found in most cancer malignancies and support tumorigenesis by suppressing immunity and promoting tumor growth. Here we identify the bromodomain (BRD) of CBP/EP300 as a critical regulator of H3K27 acetylation… read more here.

Keywords: tumor associated; h3k27 acetylation; cbp ep300; bromodomain ... See more keywords
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Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.

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recommendations! Published in 2020 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2020.112338

Abstract: Histone modifying proteins, specifically histone deacetylases (HDACs) and bromodomains, have emerged as novel promising targets for anticancer therapy. In the current work, based on available crystal structures and docking studies, we designed dual inhibitors of… read more here.

Keywords: design synthesis; evaluation dual; biological evaluation; dual targeting ... See more keywords
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Bromodomain-containing protein 4 regulates a cascade of lipid-accumulation-related genes at the transcriptional level in the 3T3-L1 white adipocyte-like cell line.

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recommendations! Published in 2020 at "European journal of pharmacology"

DOI: 10.1016/j.ejphar.2020.173351

Abstract: Our previous study demonstrated that the transfection of a short hairpin (sh)RNA targeting bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) family of proteins, into 3T3-L1 cells, a white adipocyte-like cell… read more here.

Keywords: cell line; like cell; adipocyte like; white adipocyte ... See more keywords

Evaluating the GCN5b bromodomain as a novel therapeutic target against the parasite Toxoplasma gondii.

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recommendations! Published in 2020 at "Experimental parasitology"

DOI: 10.1016/j.exppara.2020.107868

Abstract: Toxoplasma gondii is a protozoan parasite of great importance in human and veterinary health. The frontline treatment of antifolates suffers a variety of drawbacks, including toxicity and allergic reactions, underscoring the need to identify novel… read more here.

Keywords: gcn5b; toxoplasma gondii; gcn5b bromodomain; bromodomain ... See more keywords
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Selectively targeting individual bromodomain: drug discovery and molecular mechanisms.

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recommendations! Published in 2021 at "Pharmacological research"

DOI: 10.1016/j.phrs.2021.105804

Abstract: Bromodomain-containing proteins include bromodomain and extra-terminal (BET) and non-BET families. Due to the conserved bromodomain (BD) module between BD-containing proteins, and especially BETs with each member having two BDs (BD1 and BD2), the high degree… read more here.

Keywords: drug discovery; bet; selectively targeting; bromodomain ... See more keywords
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Alternative Mechanisms for DNA Engagement by BET Bromodomain-Containing Proteins.

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recommendations! Published in 2022 at "Biochemistry"

DOI: 10.1021/acs.biochem.2c00157

Abstract: Epigenetic reader domains regulate chromatin structure and modulate gene expression through the recognition of post-translational modifications on histones. Recently, reader domains have also been found to harbor double-stranded (ds) DNA-binding activity, which is as functionally… read more here.

Keywords: dna engagement; bet; mechanisms dna; bet bromodomain ... See more keywords

Bromodomain Interactions with Acetylated Histone 4 Peptides in the BRD4 Tandem Domain: Effects on Domain Dynamics and Internal Flexibility

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recommendations! Published in 2022 at "Biochemistry"

DOI: 10.1021/acs.biochem.2c00226

Abstract: The bromodomain and extra-terminal (BET) protein BRD4 regulates gene expression via recruitment of transcriptional regulatory complexes to acetylated chromatin. Like other BET proteins, BRD4 contains two bromodomains, BD1 and BD2, that can interact cooperatively with… read more here.

Keywords: histone; bd1 bd2; bromodomain; order parameters ... See more keywords