Results 51 to 60 of about 4,858 (185)
A chemical toolbox for the study of bromodomains and epigenetic signaling
Nature Communications, 2019 Bromodomains are conserved protein interaction modules that recognize acetyl-lysine modifications. Here the authors present a set of 25 selective small molecule inhibitors covering 29 human bromodomain targets and comprehensively evaluate the selectivity
Qin Wu +19 more
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Viral Hijacking of BET Proteins
Viruses, 2022 Proteins of the bromodomain and exterminal domain (BET) family mediate critical host functions such as cell proliferation, transcriptional regulation, and the innate immune response, which makes them preferred targets for viruses.
Irene P. Chen, Melanie Ott
doaj +1 more source
T Cell Exhaustion in Cancer Immunotherapy: Heterogeneity, Mechanisms, and Therapeutic Opportunities
Advanced Science, EarlyView.T cell exhaustion limits immunotherapy efficacy. This article delineates its progression from stem‐like to terminally exhausted states, governed by persistent antigen, transcription factors, epigenetics, and metabolism. It maps the exhaustion landscape in the TME and proposes integrated reversal strategies, providing a translational roadmap to overcome
Yang Yu +7 more
wiley +1 more source
Unveiling the folding mechanism of the Bromodomains
Biochemistry and Biophysics Reports, 2017 Bromodomains (BRDs) are small protein domains often present in large multidomain proteins involved in transcriptional regulation in eukaryotic cells. They currently represent valuable targets for the development of inhibitors of aberrant transcriptional ...
Maria Petrosino +6 more
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Dual Aptamers‐Based SETDB1 PROTACs as Effective Anti‐Tumor Strategies for Breast Cancer
Advanced Science, EarlyView.This study establishes dual‐aptamer PROTACs targeting SETDB1 using a SETDB1‐specific aptamer conjugated to AS1411. The designed PROTACs penetrate cells, recruit MDM2 to degrade SETDB1, and inhibit cancer cell proliferation and migration. Remarkably, they also overcome tamoxifen resistance and enhance CD8+ T cell cytotoxicity, suppressing tumor growth ...
Yanxuan Guo +6 more
wiley +1 more source
Selective BET bromodomain inhibition as an antifungal therapeutic strategy
Nature Communications, 2017 BET proteins bind chromatin through their bromodomains (BDs) to regulate transcription and chromatin remodelling. Here, the authors show that the BET protein Bdf1 is essential for the fungal pathogenCandida albicans, and report compounds that inhibit the
Flore Mietton +17 more
doaj +1 more source
Advanced Science, EarlyView.This study demonstrates that somatic PIK3CA mutations suppress PPT1 expression via activation of the PI3K–AKT–c‐JUN axis. This reduction in PPT1 weakens its interaction with P300, thereby increasing palmitoylation at C1176 of P300 and protecting P300 from lysosomal degradation.
Hongrui Chen +7 more
wiley +1 more source
DNA binding drives the association of BRG1/hBRM bromodomains with nucleosomes
Nature Communications, 2017 BRG1 and BRM are central components of the BAF (mSWI/SNF) chromatin remodelling complex, which is critical for regulation of chromatin structure. Here, the authors provide evidence that both the BRG1 and hBRM bromodomains have DNA-binding activity and ...
Emma A. Morrison +8 more
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BET Bromodomain Degradation Disrupts Function but Not 3D Formation of RNA Pol2 Clusters
Pharmaceuticals, 2023 Fusion-positive rhabdomyosarcoma (FP-RMS) is driven by a translocation that creates the chimeric transcription factor PAX3-FOXO1 (P3F), which assembles de novo super enhancers to drive high levels of transcription of other core regulatory transcription ...
Diana H. Chin +13 more
doaj +1 more source
Bromodomains: pockets with therapeutic potential
Trends in Molecular Medicine, 2014 Intense interest in the complex biology of the bromodomain (BRD) protein modules has fueled the development of novel small molecule inhibitors that target the acetyl-lysine (KAc) binding pocket of the BRD. BRD inhibition has revealed exciting opportunities for treating a variety of maladies such as cancer, inflammation, obesity, cardiovascular disease,
Papavassiliou, Kostas A. +1 more
openaire +3 more sources