ACC010, a novel BRD4 inhibitor, synergized with homoharringtonine in acute myeloid leukemia with FLT3-ITD.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular oncology"
DOI: 10.1002/1878-0261.13368
Abstract: Bromodomain-containing protein 4 (BRD4) inhibitors have been clinically developed to treat acute myeloid leukemia (AML), but their application is limited by the possibility of drug resistance, which is reportedly associated with the activation of the… read more here.
Keywords: itd; acc010; hht; brd4 ... See more keywords
Interfering with bromodomain epigenome readers as therapeutic option in mucoepidermoid carcinoma
Sign Up to like & getrecommendations! Published in 2018 at "Cellular Oncology"
DOI: 10.1007/s13402-018-0416-2
Abstract: PurposeEmerging evidence indicates that bromodomains comprise a conserved class of epigenome readers involved in cancer development and inflammation. Bromodomains are associated with epigenetic modifications of gene transcription through interactions with lysine residues of histone tails.… read more here.
Keywords: epigenome readers; mucoepidermoid carcinoma; mec; brd4 ... See more keywords
Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103817
Abstract: Bromodomain-containing protein 4 (BRD4) plays a crucial role in the epigenetic regulation of gene transcription and some BRD4 inhibitors have been advanced to clinical trials. Nevertheless, the clinical application of BRD4 inhibitors could be limited… read more here.
Keywords: pyrrolopyridone derivative; brd4 degraders; small molecule; development small ... See more keywords
An optimized BRD4 inhibitor effectively eliminates NF-κB-driven triple-negative breast cancer cells.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105158
Abstract: Acetylation of NF-κB's RelA subunit at lysine-310 (AcLys310) helps to maintain constitutive NF-κB activity in cancers such as triple-negative breast cancer (TNBC). Bromodomain-containing factor BRD4 binds to acetylated RelA to promote the activity of NF-κB.… read more here.
Keywords: acetylated rela; negative breast; breast cancer; brd4 ... See more keywords
Immature CD8 Single-Positive Thymocytes Are a Molecularly Distinct Subpopulation, Selectively Dependent on BRD4 for Their Differentiation
Sign Up to like & getrecommendations! Published in 2018 at "Cell reports"
DOI: 10.1016/j.celrep.2018.06.007
Abstract: SUMMARY T cell differentiation in the thymus proceeds in an ordered sequence of developmental events characterized by variable expression of CD4 and CD8 coreceptors. Here, we report that immature single-positive (ISP) thymocytes are molecularly distinct… read more here.
Keywords: thymocytes molecularly; subpopulation; differentiation; single positive ... See more keywords
Brd4 and P300 Confer Transcriptional Competency during Zygotic Genome Activation.
Sign Up to like & getrecommendations! Published in 2019 at "Developmental cell"
DOI: 10.1016/j.devcel.2019.05.037
Abstract: The awakening of the genome after fertilization is a cornerstone of animal development. However, the mechanisms that activate the silent genome after fertilization are poorly understood. Here, we show that transcriptional competency is regulated by… read more here.
Keywords: genome activation; brd4; transcriptional competency; p300 ... See more keywords
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.04.006
Abstract: A series of diverse small molecules have been designed and synthesized through structure-based drug design by taking advantage of fragment merging and elaboration approaches. Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and… read more here.
Keywords: potent selective; brd4 inhibitors; airway inflammation; brd4 ... See more keywords
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112780
Abstract: Bromodomain protein 4 (BRD4) plays a crucial role in transcriptional regulation and is considered to be a viable drug target for cancer treatment. Herein, we designed and synthesized a series of indole-2-one derivatives through scaffold… read more here.
Keywords: design synthesis; compound 12j; one derivatives; indole one ... See more keywords
The suppression of Brd4 inhibits peripheral plasma cell differentiation and exhibits therapeutic potential for systemic lupus erythematosus.
Sign Up to like & getrecommendations! Published in 2021 at "International immunopharmacology"
DOI: 10.1016/j.intimp.2021.108498
Abstract: The mechanisms that control B cell terminal differentiation remain undefined. Here, we investigate the role of bromodomain-containing protein 4 (Brd4) in regulating B cell differentiation and its therapeutic potential for B cell-mediated autoimmune diseases including… read more here.
Keywords: differentiation; cell; plasma cell; cell differentiation ... See more keywords
Epigenetic regulator BRD4 is involved in cadmium-induced acute kidney injury via contributing to lysosomal dysfunction, autophagy blockade and oxidative stress.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of hazardous materials"
DOI: 10.1016/j.jhazmat.2021.127110
Abstract: Cadmium (Cd) is a known nephrotoxic heavy metal and proximal tubules are the major target of Cd-induced acute kidney injury (AKI). We previously demonstrated that lysosomal dysfunction and dysregulated autophagy contribute to Cd-induced AKI. Recent… read more here.
Keywords: lysosomal dysfunction; brd4; autophagy; oxidative stress ... See more keywords
Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors
Sign Up to like & getrecommendations! Published in 2019 at "Translational Oncology"
DOI: 10.1016/j.tranon.2019.09.013
Abstract: Simultaneous inhibition of multiple molecular targets is an established strategy to improve the continuance of clinical response to therapy. Here, we screened 49 molecules with dual nanomolar inhibitory activity against BRD4 and PLK1, best classified… read more here.
Keywords: plk1; plk1 brd4; dual plk1; small molecule ... See more keywords