Results 51 to 60 of about 27,094 (219)

Epigenetic heterogeneity and plasticity in therapy‐induced tumor states through single‐cell multi‐omics

Molecular Oncology, EarlyView.
Single‐cell multi‐omics reveals epigenetic heterogeneity across therapy‐adaptive tumor states, including quiescent/dormant, drug‐tolerant persister, and EMT‐like phenotypes. By linking regulatory features with state‐associated biomarkers, these approaches inform biomarker‐guided therapeutic strategies for evolving tumors.
Hee Jung Kim, Hwiyeong Lee, Jin Hong, Daechan Park   +3 more
wiley   +1 more source

Molecular Basis for the N‑Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor

, 2018
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails are essential for maintaining cellular homeostasis. When dysregulated, “reader” proteins become drivers of disease.
John C. Widen (1951051), Joseph J. Topczewski (1323912), William C. K. Pomerantz (1476328), Jin-Yi Zhu (1319226), Ernst K. Schonbrunn (5858630), Anand Divakaran (2041456), Norbert Berndt (1319235), Daniel A. Harki (1523884), Neeraj K. Mishra (1507708), Huarui Cui (5858624), Siva K. Talluri (5858621), Alex M. Ayoub (4092883), Angela S. Carlson (5858627)   +12 more
core   +2 more sources

Targeting transcription factors associated with hemoglobinopathies: Lessons from successful interventions and implications for cancer

Molecular Oncology, EarlyView.
This review summarizes the transcription factors, repressive chromatin‐modifying complexes, and epigenetic mechanisms that control fetal hemoglobin repression. Notably, many regulators of γ‐globin silencing also function in transcriptional and epigenetic networks that drive cancer, highlighting opportunities to translate advances in hemoglobinopathy ...
Meigen Yu, Puspa Das, Xing Zhang, Xiaodong Cheng   +3 more
wiley   +1 more source

Advancements in the development of non-BET bromodomain chemical probes [PDF]

, 2019
The bromodomain and extra terminal (BET) family of bromodomain‐containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high‐quality chemical probes for their tandem bromodomains.
Tomkinson, Nicholas C. O., Prinjhal, Rab K., Clegg, Michael A., Humphreys, Philip G.   +3 more
core   +4 more sources

Histone H3K18 Lactylation Promotes the Malignant Progression of Wilms Tumor via a PSRC1/AKT/HIF‐1α Positive Feedback Loop

Advanced Science, EarlyView.
In nephroblastoma, aberrant glycolysis drives lactate accumulation, which elevates histone H3K18 lactylation via p300. Lactylation of the PSRC1 promoter activates its transcription. PSRC1 competitively binds AKT, relieving PTEN‐mediated inhibition and triggering AKT/mTOR/HIF‐1α signaling.
Yanping Wang, Hongjie Gao, Bifei Zhang, Xuetian Li, Ding Li, Aihua Cao, Fengyin Sun   +6 more
wiley   +1 more source

Targeting Tex10 Overcomes Oxaliplatin Resistance by Competitively Disrupting the Non‐Canonical BAF Complex in Colorectal Cancer

Advanced Science, EarlyView.
This study reveals that Tex10 drives oxaliplatin resistance in colorectal cancer by competitively binding BRD9 to disrupt the ncBAF complex, thereby suppressing AMBRA1 transcription and ULK1‐mediated autophagy. Gemcitabine is identified as a direct Tex10 inhibitor that restores autophagy and overcomes resistance.
Ping Xu, Jie Huang, Xiaojin Gao, Lin Deng, Yanheng Deng, Denglu Wang, Chunlei Yu, Yunxiang Zhang, Jingdong Li, Xiaocong Xiang   +9 more
wiley   +1 more source

Blocking the Bromodomains Function Contributes to Disturbances in Alga Chara vulgaris Spermatids Differentiation

Cells, 2020
Bromodomain containing (BRD) proteins play an essential role in many cellular processes. The aim of this study was to estimate activity of bromodomains during alga Chara vulgaris spermatids differentiation. The effect of a bromodomain inhibitor, JQ1 (100
Agnieszka Wojtczak
doaj   +1 more source

TRIM28‐Derived Peptide Exerts Anti‐Tumor Roles by Stabilizing Tumor Suppressive BRD7 Protein in Multiple Cancers

Advanced Science, EarlyView.
An α‐helical peptide, TAB12, designed to mimic the TRIM28 binding interface, competitively disrupts the TRIM28‐BRD7 interaction, thereby blocking ubiquitin‐mediated degradation of the tumor suppressor BRD7. This stabilization unleashes potent anti‐tumor effects across multiple tumor types with a favorable safety profile, offering a feasible strategy ...
Qingqing Wei, Changning Xue, Mengna Li, Jianxia Wei, Lemei Zheng, Shipeng Chen, Yijie Wang, Yumei Duan, Yanwei Luo, Wei Xiong, Ming Zhou   +10 more
wiley   +1 more source

High affinity binding of H3K14ac through collaboration of bromodomains 2, 4 and 5 is critical for the molecular and tumor suppressor functions of PBRM1

Molecular Oncology, 2019
Polybromo‐1 (PBRM1) is an important tumor suppressor in kidney cancer. It contains six tandem bromodomains (BDs), which are specialized structures that recognize acetyl‐lysine residues.
Lili Liao, Nilda L. Alicea‐Velázquez, Lauren Langbein, Xiaohua Niu, Weijia Cai, Eun‐Ah Cho, Meiling Zhang, Celeste B. Greer, Qin Yan, Michael S. Cosgrove, Haifeng Yang   +10 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, Min Zhu, Xinyu Tan, Yixing Zhang, Xiangning Liu, Li Yang   +5 more
doaj   +1 more source