Results 81 to 90 of about 13,555 (204)

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

Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues

ESC Heart Failure, Volume 12, Issue 2, Page 1059-1080, April 2025.
Abstract Systemic aging influences various physiological processes and contributes to structural and functional decline in cardiac tissue. These alterations include an increased incidence of left ventricular hypertrophy, a decline in left ventricular diastolic function, left atrial dilation, atrial fibrillation, myocardial fibrosis and cardiac ...
Zhuyubing Fang, Umar Raza, Jia Song, Junyan Lu, Shun Yao, Xiaohong Liu, Wei Zhang, Shujuan Li   +7 more
wiley   +1 more source

The BET/BRD inhibitor JQ1 improves brain plasticity in WT and APP mice [PDF]

Translational Psychiatry, 2017
AbstractHistone acetylation is essential for memory formation and its deregulation contributes to the pathogenesis of Alzheimer’s disease. Thus, targeting histone acetylation is discussed as a novel approach to treat dementia. The histone acetylation landscape is shaped by chromatin writer and eraser proteins, while readers link chromatin state to ...
Benito, E, Ramachandran, B, Schroeder, H, Schmidt, G, Urbanke, H, Burkhardt, S, Capece, V, Dean, C, Fischer, A   +8 more
openaire   +4 more sources

EGFR signaling confers resistance to BET inhibition in hepatocellular carcinoma through stabilizing oncogenic MYC

Journal of Experimental & Clinical Cancer Research, 2019
Background The bromodomain and extra-terminal domain (BET) inhibitor is a type of anti-tumor agent, currently being evaluated in phase I and II clinical trials for cancer therapy.
Yalei Yin, Mingju Sun, Xi Zhan, Changqing Wu, Pengyu Geng, Xiaoyan Sun, Yunsong Wu, Shuijun Zhang, Jianhua Qin, Zhengping Zhuang, Yang Liu   +10 more
doaj   +1 more source

Artificial intelligence empowers targeted protein degradation: Core technological innovations, multi‐scenario applications, and translational prospects

Smart Molecules, EarlyView.
AI is transforming TPD by improving the design, prediction, and optimization of degraders such as PROTACs, molecular glues, and LYTACs. This review summarizes key AI‐driven advances, highlights applications across drug discovery stages, and discusses remaining challenges and future directions for accelerating the development of therapies against ...
Shuanglin Qin, Rui Peng, Guangshuai Zhang, Si Yan, Jin Xiao, Zishu Liu, Ziyu Tan, Qingqing Xie, Shangjie Li, Wei Luo, Xiaohe Xiao   +10 more
wiley   +1 more source

BRD9 inhibition as potential treatment option for testicular germ cell tumors

Andrology, EarlyView.
Abstract Background Testicular germ cell tumors (TGCT) are the predominant tumor in younger males. Usually, 5‐year survival rates are quite high, but 15–20% of patients with metastatic non‐seminomas are resistant to standard cisplatin‐based therapy.
Aylin Hansen, Christine Sanders, Florian Fronhoffs, Kai Funke, Glen Kristiansen, Hubert Schorle   +5 more
wiley   +1 more source

Histone deacetylase inhibitors as venetoclax‐sensitising partners in acute myeloid leukaemia: Mechanisms, pharmacology and translational perspectives

British Journal of Pharmacology, EarlyView.
Abstract Venetoclax combined with hypomethylating agents has improved treatment for older or unfit patients with acute myeloid leukaemia (AML), but resistance and relapse remain common. This review analyses the rationale for combining venetoclax with inhibitors of histone deacetylase (HDAC).
Jaebok Lee, Marc Diederich
wiley   +1 more source

Toxicity of JQ1 in neuronal derivatives of human umbilical cord mesenchymal stem cells [PDF]

Oncotarget, 2018
Bromodomain and extra-terminal domain (BET) proteins regulate the transcription of many genes including c-MYC, a proto-oncogene, which is upregulated in many types of cancers. The thienodiazepine class of BET inhibitors, such as JQ1, inhibits growth of cancer cells and triggers apoptosis.
Bakshi, Shreeya, McKee, Christina, Walker, Keegan, Brown, Christina, Chaudhry, G. Rasul   +4 more
openaire   +2 more sources

Machine Learning‐Derived Immune Gene Signature Predicts Prognosis and Therapeutic Vulnerabilities in Multiple Myeloma

Cancer Science, EarlyView.
An immune‐related 12‐gene signature developed through integrative machine learning stratified overall survival across multiple myeloma cohorts and remained independently associated with outcome. Single‐cell, somatic mutation, and transcriptome‐based drug‐response analyses further linked the signature to multicellular bone marrow context, distinct ...
Kai Wang, Chenfei Zhao, Jingru Shi, Shiwei Liu, Yi Chen, Jujuan Wang, Zhengxu Sun, Sanmei Wang, Lei Fan, Jin Fan, Xiaoyan Qu   +10 more
wiley   +1 more source

Metabolism of JQ1, an Inhibitor of Bromodomain and Extra Terminal Bromodomain Proteins, in Human and Mouse Liver Microsomes† [PDF]

, 2020
JQ1 is a small-molecule inhibitor of the bromodomain and extra terminal (BET) protein family that potently inhibits the bromodomain testis-specific protein (BRDT), which is essential for spermatogenesis.
Santini, Conrad, Young, Damian W, Matzuk, Martin M, Li, Feng, Jain, Prashi, MacKenzie, Kevin R   +5 more
core   +1 more source