Results 201 to 210 of about 19,105 (226)
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Novel approaches to targeting BRD4
Drug Discovery Today: Technologies, 2017Inhibition of bromo and extra-terminal (BET) bromodomains, including BRD4, has emerged as a new exciting epigenetic target for oncology, in particular. Recently, novel alternatives to the traditional use of reversible small molecules have emerged, including proteolytic targeting BET agents and irreversible binding inhibitors.
Olesya A, Kharenko, Henrik C, Hansen
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Brd4: tethering, segregation and beyond
Trends in Microbiology, 2004Papillomaviruses segregate their genomes in dividing cells by tethering them to mitotic chromosomes via the viral E2 protein. A recent report has shown that this interaction is mediated by the cellular bromodomain protein Brd4. This discovery provides new insight into the mechanism of viral genome segregation and raises many exciting questions about ...
Alison A, McBride +2 more
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BRD4 and MYC—clarifying regulatory specificity
Science, 2018A study dissects the primary function of cancer-associated transcription ...
Arianna, Sabò, Bruno, Amati
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European Journal of Medicinal Chemistry, 2022
Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein. The potent degraders on MV-4-11 cells were discovered through structure-activity relationship study.
Jingjing Chen +10 more
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Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein. The potent degraders on MV-4-11 cells were discovered through structure-activity relationship study.
Jingjing Chen +10 more
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The therapeutic potential of BRD4 in cardiovascular disease
Hypertension Research, 2020Bromodomain-containing protein 4 (BRD4) is a member of the bromodomain and extra terminal (BET) protein family that has gained wide attention in the field of cancer due to its role in the formation of super enhancers (SEs) and the regulation of oncogene expression.
Shigang, Lin, Lizhong, Du
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Brd4-independence in ground state pluripotency
Nature Cell Biology, 2018Brd4, a reader of histone acetylation, is a transcriptional co-activator implicated in the maintenance of embryonic stem cells (ESCs). A study now shows that Brd4 is dispensable in mouse ESCs maintained in ground state pluripotency, and that cooperative activity of Tet1/2 and ESC-specific transcription factors compensates for its loss.
Atlasi, Y., Stunnenberg, H.G.
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An Overview on Small Molecule Inhibitors of BRD4
Mini-Reviews in Medicinal Chemistry, 2016BRD4, an epigenetic regulator that recognizes and binds the acetylated lysine residues in histone, has been reported as a potential therapeutic target for cancers. Since the first BRD4 inhibitor JQ1 developed in 2010, numerous BRD4 inhibitors have been discovered in past five years.
Wenhai, Huang +4 more
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BRD4: epigenetic origin and target of CTCL
Blood, 2018In this issue of Blood , Kohnken et al demonstrate a novel oncogenic pathway featuring IL-15-miR-29b-BRD4 positive feedback loop and targeting bromodomain-containing protein 4 (BRD4) disables the oncogenic loop, identifying a potentially effective target for therapy for cutaneous T-cell lymphoma (CTCL) patients ...
Xiaohong Zhao, Jianguo Tao
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Redistributing BRD4 in inflammation
Science-Business eXchange, 2014A new link between inflammation and atherosclerosis centers on the BET bromodomain protein BRD4 and could provide new targets for intervention.
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Distinct layers of BRD4-PTEFb reveal bromodomain-independent function in transcriptional regulation
Molecular Cell, 2023Sarah Gold +2 more
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