Results 21 to 30 of about 19,105 (226)
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
Journal of Enzyme Inhibition and Medicinal Chemistry, 2021 Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on the N-terminal tails of histones through two bromodomains (BD1 and BD2) to regulate gene transcription.
Jiao Li +9 more
doaj +1 more source
Super-enhancers and the super-enhancer reader BRD4: tumorigenic factors and therapeutic targets
Cell Death Discovery, 2023 Transcriptional super-enhancers and the BET bromodomain protein BRD4 are emerging as critical drivers of tumorigenesis and therapeutic targets. Characterized by substantial accumulation of histone H3 lysine 27 acetylation (H3K27ac) signals at the loci of
Haihong Qian +5 more
doaj +1 more source
Bromodomain protein BRD4 is an epigenetic activator of B7-H6 expression in acute myeloid leukemia
OncoImmunology, 2021 B7-H6, a ligand for the NK activating receptor NKp30, has been identified as a biomarker of poor prognosis in several solid cancers. However, little is known about the role of B7-H6 and the mechanisms that control its expression in acute myeloid leukemia
Aroa Baragaño Raneros +7 more
doaj +1 more source
Genes & Cancer, 2023 Chemoresistance in ovarian carcinoma is a puzzling issue that urges understanding of strategies used by cancer cells to survive DNA damage and to escape cell death. Expanding efforts to understand mechanisms driving chemoresistance and to develop alternative therapies targeting chemoresistant tumors are critical.
Drumond-Bock, Ana Luiza +6 more
openaire +2 more sources
Inducing DNA damage through R-loops to kill cancer cells
Molecular & Cellular Oncology, 2021 R-loops are intermediate structures of transcription that can accumulate when transcriptional elongation is blocked by inhibiting BRD4. In normal cells, R-loop persistence suppresses firing of adjacent replication origins.
Fred C. Lam +2 more
doaj +1 more source
Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader
, 2021 Targeted protein degradation is a powerful induced-proximity tool to control cellular concentrations of native proteins using small molecules. However, the design of selectivity in protein degradation remains challenging.
Huda, Zahid +5 more
core +1 more source
Regulation of programmed cell death by Brd4
Cell Death & Disease, 2022 AbstractEpigenetic factor Brd4 has emerged as a key regulator of cancer cell proliferation. Targeted inhibition of Brd4 suppresses growth and induces apoptosis of various cancer cells. In addition to apoptosis, Brd4 has also been shown to regulate several other forms of programmed cell death (PCD), including autophagy, necroptosis, pyroptosis, and ...
Jinfeng Hu +4 more
openaire +3 more sources
BRD4 as a Therapeutic Target in Pulmonary Diseases
International Journal of Molecular Sciences, 2023 Bromodomain and extra-terminal domain (BET) proteins are epigenetic modulators that regulate gene transcription through interacting with acetylated lysine residues of histone proteins. BET proteins have multiple roles in regulating key cellular functions such as cell proliferation, differentiation, inflammation, oxidative and redox balance, and immune ...
Xia Guo +4 more
openaire +2 more sources
Disease-associated Brd4 mutation – linking chromatin binding and the DNA damage response [PDF]
, 2019 Acetylation of lysine residues is a histone modification associated with active chromatin. The modified residues provide docking sites for the epigenetic reader BRD4, which binds to the acetylated lysines via its two bromodomains.
Olley, Gabrielle Jade
core +1 more source