Results 51 to 60 of about 19,105 (226)

LncRNA UCA1 Accelerates the Progression of Ulcerative Colitis via Mediating the miR-331-3p/BRD4 Axis

International Journal of General Medicine, 2021
Jun Rao, Lihua Shao, Min Lin, Jin Huang, Li Fan Department of Gastroenterology, The Affiliated Changzhou No.2 People’s Hospital of Nanjing Medical University, Changzhou, People’s Republic of ChinaCorrespondence: Li FanDepartment of ...
Rao J, Shao L, Lin M, Huang J, Fan L
doaj  

The Bromodomain Protein 4 Contributes to the Regulation of Alternative Splicing

Cell Reports, 2019
Summary: The bromodomain protein 4 (BRD4) is an atypical kinase and histone acetyl transferase (HAT) that binds to acetylated histones and contributes to chromatin remodeling and early transcriptional elongation.
Sheetal Uppal, Anne Gegonne, Qingrong Chen, Petria S. Thompson, Dan Cheng, Jie Mu, Daoud Meerzaman, Hari S. Misra, Dinah S. Singer   +8 more
doaj   +1 more source

BRD4 Structure–Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536 [PDF]

ACS Medicinal Chemistry Letters, 2015
A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities. Particularly, replacement of the cyclopentyl group with a 3-bromobenzyl moiety afforded the most potent BRD4 inhibitor of the series (39j) with a K i = 8.7 nM, which was equipotent against ...
Lijia, Chen, Jeremy L, Yap, Makoto, Yoshioka, Maryanna E, Lanning, Rachel N, Fountain, Mithun, Raje, Jacob A, Scheenstra, Jeffrey W, Strovel, Steven, Fletcher   +8 more
openaire   +2 more sources

BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes

Cancer Biology & Therapy, 2022
Acute myeloid leukemia (AML) is a highly cancerous and aggressive hematologic disease with elevated levels of drug resistance and relapse resulting in high mortality.
Li Ma, Jianwei Wang, Yongping Zhang, Fang Fang, Jing Ling, Xinran Chu, Zimu Zhang, Yanfang Tao, Xiaolu Li, Yuanyuan Tian, Zhiheng Li, Xu Sang, Kunlong Zhang, Lihui Lu, Xiaomei Wan, Yanling Chen, Juanjuan Yu, Ran Zhuo, Shuiyan Wu, Jun Lu, Jian Pan, Shaoyan Hu   +21 more
doaj   +1 more source

BRD4 isoforms have distinct roles in tumour progression and metastasis in rhabdomyosarcoma

EMBO Reports
BRD4, a bromodomain and extraterminal (BET) protein, is deregulated in multiple cancers and has emerged as a promising drug target. However, the function of the two main BRD4 isoforms (BRD4-L and BRD4-S) has not been analysed in parallel in most cancers.
Dipanwita Das, Jia Yu Leung, Shivaranjani Balamurugan, Vinay Tergaonkar, Amos Hong Pheng Loh, Cheng-Ming Chiang, Reshma Taneja   +6 more
doaj   +1 more source

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

Enhancer remodeling regulates epigenetic adaptation and resistance to MEK1/2 inhibition in triple-negative breast cancer

Molecular & Cellular Oncology, 2017
Kinase inhibitors targeting the mitogen/extracellular signal-regulated kinase kinase (MEK)- extracellular signal related kinase (ERK) signaling pathway have limited durability in inhibiting growth of triple-negative breast cancer.
Samantha M. Bevill, Jon S. Zawistowski, Gary L. Johnson   +2 more
doaj   +1 more source

DNA Damage Induces Dynamic Associations of BRD4/P-TEFb With Chromatin and Modulates Gene Transcription in a BRD4-Dependent and -Independent Manner

Frontiers in Molecular Biosciences, 2020
The bromodomain-containing protein BRD4 has been thought to transmit epigenetic information across cell divisions by binding to both mitotic chromosomes and interphase chromatin. UV-released BRD4 mediates the recruitment of active P-TEFb to the promoter,
Yawei Song, Yawei Song, Yawei Song, Yawei Song, Yawei Song, Gongcheng Hu, Gongcheng Hu, Gongcheng Hu, Gongcheng Hu, Jinping Jia, Mingze Yao, Xiaoshan Wang, Wenliang Lu, Andrew P. Hutchins, Jiekai Chen, Jiekai Chen, Jiekai Chen, Keiko Ozato, Hongjie Yao, Hongjie Yao, Hongjie Yao, Hongjie Yao   +21 more
doaj   +1 more source

ZW4864‐mediated inhibition of the β‐catenin/BCL9/BCL9L complex reveals therapeutic potential in bladder cancer

Molecular Oncology, EarlyView.
BCL9 and BCL9L drive bladder cancer progression by enhancing β‐catenin signaling, promoting proliferation, migration, invasion, and organoid growth. Genetic depletion of BCL9(L) suppresses malignant phenotypes, while pharmacological disruption of the β‐catenin/BCL9(L) complex with ZW4864 inhibits canonical Wnt signaling and tumor‐associated cellular ...
Roland Kotolloshi, Mandy Berndt‐Paetz, Eileen Lerner, Gregoire Najjar, Anca Azoitei, Krishna Pal Singh, Shailendra Kumar Gupta, Olaf Wolkenhauer, Cagatay Günes, Otmar Huber, Marc‐Oliver Grimm, Daniel Steinbach   +11 more
wiley   +1 more source

Discovery of an Unexpected Similarity in Ligand Binding Between BRD4 and PPARγ

, 2019
Knowledge about interrelationships between different proteins is crucial in fundamental research for the elucidation of protein networks and pathways.
Jette, Pretzel, Oliver, Koch, Saskia, Spitzer, Lina, Humbeck   +3 more
core   +1 more source