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Brd4 associates with mitotic chromosomes throughout early zebrafish embryogenesis
MS645 blocks BRD4 binding to transcription enhancer/mediator proteins MED1 (zeige MED1 Proteine) and YY1 (zeige YY1 Proteine) with potency superior to monovalent BET inhibitors, resulting in down-regulation of proinflammatory cytokines and genes for cell-cycle control and DNA damage repair that are largely unaffected by monovalent BrD inhibition.
Study shows that BRD4 is significantly highly expressed in gastric cancer patients and cell lines and positively regulates the expression of c-MYC (zeige MYC Proteine) through transcription regulation and epigenetic levels. Functionally, these result demonstrate that the knockdown of BRD4 represses the proliferation and induces the apoptosis of gastric cancer cells through repression of c-MYC (zeige MYC Proteine).
BRD4 hyperphosphorylation is associated with cellular transformation in NUT midline carcinoma
Results suggest structure-based drug design of bromodomain-containing protein 4 (Brd4) inhibitors.
Cells harboring the fusion gene are selectively sensitive to small-molecule inhibition of protein targets induced by, or bound to, PAX3 (zeige PAX3 Proteine)-FOXO1 (zeige FOXO1 Proteine)-occupied super enhancers. Furthermore, PAX3 (zeige PAX3 Proteine)-FOXO1 (zeige FOXO1 Proteine) recruits and requires the BET bromodomain protein BRD4 to function at super enhancers, resulting in a complete dependence on BRD4 and a significant susceptibility to BRD inhibition
Our data suggested that downregulation of BRD4 in gallbladder cancer (GBC) cells induced apoptosis by PI3K (zeige PIK3CA Proteine)/AKT (zeige AKT1 Proteine) pathway. Inhibition of BRD4 expression may be a novel therapeutic strategy for patients with GBC.
these results highlighted the significant genetic contribution of the ARID1B variant, rs73013281, to susceptibility for HCC (zeige FAM126A Proteine), especially in interaction with physical activity.
In pluripotent cells, Brd2 (zeige BRD2 Proteine)-Brd4 occupy Nodal gene regulatory elements (NREs), but only Brd4 is required for pluripotency gene expression. Brd4 downregulation facilitates pluripotent exit and drives enhanced Brd2 (zeige BRD2 Proteine) NRE occupancy, thereby unveiling a specific function for Brd2 (zeige BRD2 Proteine) in differentiative Nodal-Smad2 (zeige SMAD2 Proteine) signalling
Findings reveal that PCa (zeige FLVCR1 Proteine)-associated ERG (zeige ERG Proteine) can interact and co-occupy with BRD4 in the genome, and suggest this druggable interaction is critical for ERG (zeige ERG Proteine)-mediated cell invasion and PCa (zeige FLVCR1 Proteine) progression.
Our data strongly support the use of CCR2 (zeige CCR2 Proteine) and CD180 (zeige CD180 Proteine) mRNAs as whole blood pharmacodynamic (PD)biomarkers for BRD4 inhibitors, especially in situations where paired tumor biopsies are unavailable. In addition, they can be used as tumor-based PD biomarkers for hematologic tumors.
results suggest that rhythmic expression of Sglt1 (zeige SLC5A1 Proteine) is regulated at the mRNA transcriptional elongation level by enhancing the binding of the BRD4-P-TEFb (zeige CCNT1 Proteine) complex to acetylated histones at the gene upon BMAL1 (zeige ARNTL Proteine)-CLOCK binding to Sglt1 (zeige SLC5A1 Proteine)
Bromodomain protein BRD4 promotes cell proliferation in skin squamous cell carcinoma.
By modulating the translation of IkappaBalpha (zeige NFKBIA Proteine) via the Mnk2 (zeige MKNK2 Proteine)-eIF4E (zeige EIF4E Proteine) pathway, Brd4 provides an additional layer of control for NF-kappaB (zeige NFKB1 Proteine)-dependent inflammatory gene expression and inflammatory response.
Using compound selectivity engineering and CRISPR/Cas9 genome editing, distinct functions for Erk5 (zeige MAPK7 Proteine) and Brd4 in pluripotency regulation of mouse embryonic stem cells have been revealed.
Long-term treatment with bromodomain-containing protein 4 (BRD4) inhibitors caused telomere shortening in both mouse and human cells, suggesting BRD4 plays a role in telomere maintenance in vivo.
Fmr1 (zeige FMR1 Proteine) knockout (KO) mice show widespread changes in histone marks as well as transcriptional misregulation resulting in increased expression of many critical synaptic genes. Data suggest that one chromatin target of FMRP (zeige FMR1 Proteine), the reader protein Brd4, appears to be significantly involved in this transcriptional disruption.
The functional domains of mouse BRD4 and its role in transcription are described. Review.
Brd2 (zeige BRD2 Proteine) and Brd4 genetic transcription required for Th17 cell development and adaptive immunity.
These data provide a detailed mechanism for how activated NF-kappaB (zeige NFKB1 Proteine) and BRD4 control epithelial-mesenchymal transition initiation and transcriptional elongation in model airway epithelial cells in vitro and in a murine pulmonary fibrosis model in vivo.
DOT1L (zeige DOT1L Proteine), via dimethylated histone H3 (zeige HIST3H3 Proteine) K79, facilitates histone H4 acetylation, which in turn regulates the binding of BRD4 to chromatin in acute lymphoblastic leukemia.
The protein encoded by this gene is homologous to the murine protein MCAP, which associates with chromosomes during mitosis, and to the human RING3 protein, a serine/threonine kinase. Each of these proteins contains two bromodomains, a conserved sequence motif which may be involved in chromatin targeting. This gene has been implicated as the chromosome 19 target of translocation t(15\;19)(q13\;p13.1), which defines an upper respiratory tract carcinoma in young people. Two alternatively spliced transcript variants have been described.
Bromodomain-containing protein 4B
, bromodomain-containing protein 4B
, bromodomain containing 4
, bromodomain-containing protein 4
, bromodomain 4
, bromodomain-containing protein 4-like
, bromodomain containing protein 4
, bromodomain-containing 4
, chromosome-associated protein
, bromodomain-containing 5
, fsh-like protein
, mitotic chromosome-associated protein