Interrogating Histone Acetylation and BRD4 as Mitotic Bookmarks of Transcription
Cell Reports, 2019 Summary: Global changes in chromatin organization and the cessation of transcription during mitosis are thought to challenge the resumption of appropriate transcription patterns after mitosis.
Cheryl A Keller +2 more
exaly +4 more sources
The poly(ADP-ribosyl)ation of BRD4 mediated by PARP1 promoted pathological cardiac hypertrophy
Acta Pharmaceutica Sinica B, 2021 The bromodomain and extraterminal (BET) family member BRD4 is pivotal in the pathogenesis of cardiac hypertrophy. BRD4 induces hypertrophic gene expression by binding to the acetylated chromatin, facilitating the phosphorylation of RNA polymerases II ...
Min Liu, Zhuoming Li, Junjian Wang
exaly +3 more sources
Glucose and Glutamine Deprivation Promotes Breast Cancer Lung Metastasis via BRD4-Dependent Enhancer Activation. [PDF]
Adv Sci (Weinh)To model a nutrient‐restricted tumor microenvironment, breast cancer cells were adapted to low glucose and glutamine levels. In the adapted cells, BRD4‐driven enhancer activation increases pro‐invasive EDN1 expression, facilitated by ATF3/c‐JUN and reinforced by enhancer RNA.
Bhattarai PY +4 more
europepmc +2 more sources
In Situ Bioorthogonal Synthesis of PROTACs via Dual-Responsive Cleavage for Synergistic Photo-Immunotherapy. [PDF]
Adv Sci (Weinh)A bioactive self‐delivering SNAP‐TAC platform responds to tumor‐associated cathepsin B and glutathione, enabling in situ bioorthogonal synthesis of a BRD4‐degrading proteolysis‐targeting chimera within the tumor microenvironment. The resulting BRD4 degradation and PD‐L1 downregulation synergize with photodynamic therapy‐induced immunogenic cell death ...
Jian S +14 more
europepmc +2 more sources
Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation. [PDF]
Adv Sci (Weinh)Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Liu K +8 more
europepmc +2 more sources
Generalizable Strategies for the Synthesis of Cereblon-Recruiting PROTAC Prodrugs. [PDF]
Angew Chem Int Ed EnglCereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Wang AX +7 more
europepmc +3 more sources
BRD4 modulates antimicrobial defense via non-canonical NRF2 activation in macrophages to confer protection against sepsis. [PDF]
PLoS PathogensSepsis is a life-threatening condition characterized by dysregulated immune responses and high mortality, driven by persistent pathogens and compromised antimicrobial defenses.
Jinfeng Hu +16 more
doaj +2 more sources
Molecular Cancer, 2021 High-grade serous ovarian carcinoma (HGSOC) is the most aggressive type of ovarian cancer, often diagnosed at advanced stages. Molecularly, HGSOC shows high degree of genomic instability associated with large number of genetic alterations.
Ana Luiza Drumond-Bock +1 more
doaj +1 more source
BRD4 promotes heterotopic ossification through upregulation of LncRNA MANCR
Bone & Joint Research, 2021 Aims: Acquired heterotopic ossification (HO) is a debilitating disease characterized by abnormal extraskeletal bone formation within soft-tissues after injury. The exact pathogenesis of HO remains unknown.
Lei Liu +9 more
doaj +1 more source
The iterative application of a large chemical space in the drug discovery process
Журнал органічної та фармацевтичної хімії, 2021 Aim. To demonstrate the advantages of large-scale virtual libraries generated using chemical protocols previously validated in primary steps of the drug discovery process. Results and discussion.
Olena V. Savych +7 more
doaj +1 more source