Results 81 to 90 of about 14,237 (205)
Blocking SETD2 Enhances the Therapeutic Efficiency of Menin Inhibitor in MLL‐Fusion Leukemia
Combined SETD2 and menin inhibitors make synergistic effects against MLL‐fusion leukemia; the combination therapy reduces the expression of target genes through blocking transcription elongation and initiation. ABSTRACT During transcriptional elongation, the histone methyltransferase SETD2 binds to RNA polymerase II and deposits trimethylation marks at
Anpei Li +10 more
wiley +1 more source
The BET/BRD inhibitor JQ1 improves brain plasticity in WT and APP mice [PDF]
AbstractHistone acetylation is essential for memory formation and its deregulation contributes to the pathogenesis of Alzheimer’s disease. Thus, targeting histone acetylation is discussed as a novel approach to treat dementia. The histone acetylation landscape is shaped by chromatin writer and eraser proteins, while readers link chromatin state to ...
Benito, E +8 more
openaire +4 more sources
The function of bromodomain‐containing proteins in regulating gene transcription is reviewed here, including the development of chemical probes and targeted protein degradation modalities (e.g., PROTACs). This extends to clinical efforts targeting the BET bromodomain‐containing proteins. Challenges of selectivity, future prospects, and the differential
Cole R. Scholtz, William C. K. Pomerantz
wiley +1 more source
Purpose: Bromodomain and extraterminal domain (BET) inhibitors are promising epigenetic agents for the treatment of various subsets of acute myeloid leukemia (AML).
민유홍 +4 more
core +1 more source
Multiple myeloma: A tale of deregulated transcription factors
Abstract A comprehensive understanding of the molecular mechanisms underlying multiple myeloma (MM) pathogenesis is essential for developing therapeutic strategies that overcome disease heterogeneity and treatment relapse. In this review, we focus on transcription factors (TFs), key regulators of gene expression that play critical roles in normal ...
Nahia Gómez‐Echarte +5 more
wiley +1 more source
Integrating Oncolytic Virus Engineering and Delivery Strategies for Enhanced Cancer Virotherapy
Integrated engineering strategies combining oncolytic virus (OV) design with advanced delivery platforms overcome biological barriers and enhance cancer virotherapy. Genetic engineering improves viral potency and selectivity, while local and systemic delivery systems promote viral protection, tumor targeting, penetration, and tumor microenvironment ...
Jiliang Zhao +5 more
wiley +1 more source
JQ1 suppresses tumor growth via PTEN/PI3K/AKT pathway in endometrial cancer
Overexpression of c-Myc is associated with worse outcomes in endometrial cancer, indicating that c-Myc may be a promising target for endometrial cancer therapy.
Clark, Leslie H. +9 more
core +1 more source
JQ1, a small cell-permeable molecule is known for its potent inhibitory action on bromodomain and extraterminal (BET) proteins. Although earlier studies have shown its inhibitory effect on male gametogenesis, limited information is available about its ...
Keerthana Karunakar Poojary +12 more
doaj +1 more source
JQ1 increases BRD4 complex interaction with viral gene promoters.
HeLa cell were infected with HSV-1 at 10 MOI in the absence or presence of 500 nM JQ1 for 6 hr. Protein association and their interaction with viral gene promoters were determined by immunoprecipitation, by immunostaining, and by ChIP assays ...
Ke Ren (34504) +8 more
core +1 more source
Effects of bromodomain and extra-terminal inhibitor JQ1 and interleukin-6 on breast cancer cells
Background: Bromodomain and extra-terminal (BET) proteins are recognized acetylated lysine of histone 4 and act as scaffolds to recruit many other proteins to promoters and enhancers of active genes, especially at the super-enhancers of key genes ...
Jami, Mohammad-Saeid +17 more
core +1 more source

