Results 61 to 70 of about 14,237 (205)

Harnessing MDM2‐Mediated Targeted Degradation of Transcriptional and Epigenetic Machinery to Disrupt Oncogenic Addictions in Pediatric Sarcoma

open access: yesAdvanced Science, EarlyView.
MDM2 dependency in pediatric sarcomas is driven by a novel p53‐independent oncogenic cistrome alongside canonical p53 pathway suppression. This study introduces MDM2‐recruiting transcriptional and epigenetic machinery degraders (MDM2‐TEMADs) as a novel precision oncology modality.
Jiawei Zhou   +21 more
wiley   +1 more source

BET Inhibitor JQ1 Attenuates Atrial Fibrillation Through Modulation of Fibrosis, Calcium Homeostasis, and Mitochondrial Function in a Murine Model. [PDF]

open access: yesInt J Mol Sci
Bromodomain and extraterminal domain (BET) proteins act as epigenetic regulators of gene transcription. BET inhibitors have shown therapeutic potential in various models of heart failure; however, their efficacy in atrial fibrillation (AF) remains ...
Song Z   +7 more
europepmc   +2 more sources

Synthesis and biological profiling of (+)-JQ1 amides as BET inhibitors

open access: yes, 2021
BET proteini su epigenetski biološki targeti koji regulišu ekspresiju gena i uključeni su u patogenezu kancera. Jedan od inhibitora ovih proteina koji je opisan u literaturi je derivat tienotriazolodiazepina (+)-JQ1.
Koravović, Mladen   +6 more
core  

Stem Cell Differentiation Disperses Transcriptional Clusters via a Conserved Surface‐Condensate Trajectory

open access: yesAdvanced Science, EarlyView.
Stem cell differentiation follows a conserved surface condensate trajectory: H3K27ac super enhancers nucleate large RNA polymerase II clusters that grow and unfold before transcriptional activity disperses them. This work reveals how biophysical forces at enhancer surfaces dynamically build and dismantle stem cell transcription hubs, reshaping cell ...
Tim Klingberg   +18 more
wiley   +1 more source

A Pancreatitis‐Inspired Trypsinogen Nanoplatform Reprograms Tumor‐Associated Macrophages via NF‐κB for Pancreatic Cancer Immunotherapy

open access: yesAdvanced Science, EarlyView.
Trypsinogen‐loaded nanoparticles reprogram TAMs via NF‐κB/NLRP3, driving M2→M1 conversion and potent phagocytosis to unleash antitumor immunity. ABSTRACT Although reprogramming tumor‐associated macrophages (TAMs) represents a promising therapeutic strategy, approaches that are both precise and safe remain scarce.
Lei Cao   +7 more
wiley   +1 more source

BET Protein Inhibitor JQ1 Ameliorates Experimental Peritoneal Damage by Inhibition of Inflammation and Oxidative Stress

open access: yesAntioxidants, 2023
Peritoneal dialysis (PD) is a current replacement therapy for end-stage kidney diseases (ESKDs). However, long-term exposure to PD fluids may lead to damage of the peritoneal membrane (PM) through mechanisms involving the activation of the inflammatory ...
Vanessa Marchant   +13 more
doaj   +1 more source

The BET-bromodomain inhibitor JQ1 mitigates vemurafenib drug resistance in melanoma

open access: yesMelanoma Research, 2018
Inhibition of BRAF improves therapeutic efficacy of BRAF-mutant melanoma. However, drug resistance to BRAF inhibitor is inevitable, and the drug resistance mechanisms still remain to be elucidated. Here, BRAFV600E mutant cells A375 and SK-MEL-28 were chosen and treated with BRAF inhibitor vemurafenib, and the results showed that the ERK signaling ...
Zhao, Bei, Cheng, Xiankui, Zhou, Xiyuan
openaire   +3 more sources

JQ1 enhances the effects of HDAC3 depletion.

open access: yes, 2014
A significant increase in GFP protein expression from the HIV-1 promoter was observed in 2D10 cells that had been depleted of HDAC3 and had been treated with JQ1 (50 nM) for 24 hours over cells that were transduced with the scrambled shRNA control and ...
Kirston M. Barton (618002)   +8 more
core   +1 more source

The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma [PDF]

open access: yesMolecular Cancer Therapeutics, 2016
Abstract The bromodomain and extra-terminal domain inhibitor JQ1 has marked antitumor activity against several hematologic malignancies as well as solid tumor models. Here, we investigated its activity in vitro and in vivo against models of childhood rhabdomyosarcoma and Ewing sarcoma.
Hemant K, Bid   +8 more
openaire   +2 more sources

Correction: Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells

open access: yesPLOS ONE, 2015
There is an error in Fig 2 that appears to have occurred during the preparation of files after the manuscript was accepted. In Fig 2B, the blot for Brd4 incorrectly appears as a duplicate of P-Brd4. The authors have provided a corrected version of Fig 2 here. Fig 2 Brd4 occupancy and expression in different cells.
Trent Fowler   +8 more
openaire   +3 more sources

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