Results 51 to 60 of about 15,581 (231)
Epigenetic roulette in blood stream plasmodium: gambling on sex [PDF]
, 2016 No abstract ...
Waters, Andrew
core +2 more sources
Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma [PDF]
Clinical Cancer Research, 2013 Abstract Purpose: Glioblastoma is refractory to conventional therapies. The bromodomain and extraterminal domain (BET) proteins are epigenetic readers that selectively bind to acetylated lysine residues on histone tails. These proteins recently emerged as important therapeutic targets in NUT midline carcinoma and several types of ...
Cheng, Z +9 more
openaire +4 more sources
Segmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase A.
PLoS ONE, 2016 Bromodomain and extra-terminal (BET) family of proteins are one of the major readers of epigenetic marks and an important target class in oncology and other disease areas. The importance of the BET family of proteins is manifested by the explosion in the
Felix P Williams +3 more
doaj +1 more source
Biomolecules, 2018 Flavonoids are widely recognized as natural polydrugs, given their anti-inflammatory, antioxidant, sedative, and antineoplastic activities. Recently, different studies showed that flavonoids have the potential to inhibit bromodomain and extraterminal ...
Fernando D. Prieto-Martínez +1 more
doaj +1 more source
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology [PDF]
, 2016 Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains, the readers of acetyl-lysine modifications.
Alessio Ciulli +3 more
core +2 more sources
Targeting BET bromodomain proteins in solid tumors
Oncotarget, 2016 There is increasing interest in inhibitors targeting BET (bromodomain and extra-terminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression
Sahai, Vaibhav +4 more
openaire +4 more sources
BET Bromodomain Inhibition Suppresses Human T Cell Function [PDF]
ImmunoHorizons, 2019 Abstract Bromodomain and extraterminal domain (BET) proteins help direct the differentiation of helper T cell subsets, but their role in activated T cell function has not been described in detail. In this study, we investigate various consequences of epigenetic perturbation in human T lymphocytes using MK-8628, a potent and highly ...
Peter Georgiev +7 more
openaire +2 more sources
Discovery of SKP2‐Recruiting PROTACs for Target Protein Degradation
Advanced Science, EarlyView.Based on the SKP2‐targeting ligand SL1, we designed non‐covalent PROTACs by linking it with the BRD4 inhibitor JQ1 and the AR antagonist AL through a linker. These PROTACs successfully induced the ubiquitination of BRD4 and AR, followed by proteasome‐mediated degradation.
Guanjun Dong +13 more
wiley +1 more source
Viruses, 2023 Feline leukemia virus (FeLV) is a cosmopolitan gammaretrovirus that causes lifelong infections and fatal diseases, including leukemias, lymphomas, immunodeficiencies, and anemias, in domestic and wild felids.
Garrick M. Moll +2 more
doaj +1 more source
BET bromodomain proteins regulate enhancer function during adipogenesis [PDF]
Proceedings of the National Academy of Sciences, 2018 Developmental transitions are guided by master regulatory transcription factors. During adipogenesis, a transcriptional cascade culminates in the expression of PPARγ and C/EBPα, which orchestrate activation of the adipocyte gene expression program.
Jonathan D. Brown +13 more
openaire +4 more sources