Results 71 to 80 of about 43,525 (155)

The emerging role of BET inhibitors in breast cancer

Breast, 2020
Bromodomain and extraterminal domain (BET) proteins are epigenetic molecules that regulate the expression of multiple genes involved in carcinogenesis.
Angeliki Andrikopoulou, Michalis Liontos, Konstantinos Koutsoukos, Meletios-Athanasios Dimopoulos, Flora Zagouri   +4 more
doaj   +1 more source

Bromodomain and Extra Terminal (BET) Inhibitor Suppresses Macrophage-Driven Steroid-Resistant Exacerbations of Airway Hyper-Responsiveness and Inflammation. [PDF]

PLoS ONE, 2016
Exacerbations of asthma are linked to significant decline in lung function and are often poorly controlled by corticosteroid treatment. Clinical investigations indicate that viral and bacterial infections play crucial roles in the onset of steroid ...
Thi Hiep Nguyen, Steven Maltby, Fiona Eyers, Paul S Foster, Ming Yang   +4 more
doaj   +1 more source

Erythropoiesis provides a BRD's eye view of BET protein function [PDF]

Drug Discovery Today: Technologies, 2016
Pharmacologic inhibitors of the bromodomain and extra-terminal motif (BET) protein family are in clinical trials for the treatment of hematologic malignancies, yet the functions of individual BET proteins remain largely uncharacterized. We review the molecular roles of BETs in the context of erythropoiesis.
Aaron J, Stonestrom, Sarah C, Hsu, Michael T, Werner, Gerd A, Blobel   +3 more
openaire   +2 more sources

BET-Inhibitors Disrupt Rad21-Dependent Conformational Control of KSHV Latency.

, 2017
Kaposi's Sarcoma-associated Herpesvirus (KSHV) establishes stable latent infection in B-lymphocytes and pleural effusion lymphomas (PELs). During latency, the viral genome persists as an epigenetically constrained episome with restricted gene expression ...
Alessandra De Leo, Paul M Lieberman, Horng-Shen Chen (473322), Zhuo Wang, Horng-Shen Chen, Robert Hills (3685870), Paul M. Lieberman (56113), Andrew Kerekovic, Robert Hills, Zhuo Wang (18668), Alessandra De Leo (3685876), Andrew Kerekovic (3685873)   +11 more
core   +1 more source

Dual inhibition of BET and HAT/p300 suppresses colorectal cancer via DR5- and p53/PUMA-mediated cell death

Frontiers in Oncology, 2022
BackgroundColorectal cancer (CRC) frequently has a dysregulated epigenome causing aberrant up-regulation of oncogenes such as c-MYC. Bromodomain and extra-terminal domain (BET) proteins and histone acetyltransferases (HAT) are epigenetic regulatory ...
Chaoyuan Kuang, Chaoyuan Kuang, Jingshan Tong, Jingshan Tong, Kaylee Ermine, Kaylee Ermine, Manbo Cai, Manbo Cai, Fujun Dai, Fujun Dai, Suisui Hao, Suisui Hao, Francis Giles, Yi Huang, Yi Huang, Jian Yu, Jian Yu, Lin Zhang, Lin Zhang   +18 more
doaj   +1 more source

BET degrader exhibits lower antiproliferative activity than its inhibitor via EGR1 recruiting septins to promote E2F1-3 transcription in triple-negative breast cancer

Pharmacological Research
The bromodomain and extraterminal domain (BET) family proteins serve as primary readers of acetylated lysine residues and play crucial roles in cell proliferation and differentiation.
Nan Liu, Shuai Wang, Munan Li, Nan Zhao, Deyu Wang, Rui Zhang, Mingxin Yu, Luoyi Zhao, Siwei Zhang, Fangbin Han, Ying Zhao, Quan Liu   +11 more
doaj   +1 more source

EWS/ETS-Driven Ewing Sarcoma Requires BET Bromodomain Proteins

, 2018
The EWS/ETS fusion transcription factors drive Ewing sarcoma (EWS) by orchestrating an oncogenic transcription program. Therapeutic targeting of EWS/ETS has been unsuccessful; however, identifying mediators of the EWS/ETS function could offer new ...
Vijaya L. Dommeti, Aishwarya Pawar, Kari Wilder-Romans, Carl G. Engelke, Archana Nallasivam, Ramakrishnan Natesan, Felix Y. Feng, Ingrid J. Apel, Paradesi Naidu Gollavilli, Zhaohui S. Qin, Tianlei Xu, Irfan A. Asangani, Pranathi M. Krishnamurthy   +12 more
core   +1 more source

BET proteins in abnormal metabolism, inflammation, and the breast cancer microenvironment. [PDF]

J Leukoc Biol, 2018
Abstract Obesity and its associated pathology Type 2 diabetes are two chronic metabolic and inflammatory diseases that promote breast cancer progression, metastasis, and poor outcomes. Emerging critical opinion considers unresolved inflammation and abnormal metabolism separately from obesity; settings where they do not co-occur can ...
Andrieu GP, Shafran JS, Deeney JT, Bharadwaj KR, Rangarajan A, Denis GV.   +5 more
europepmc   +5 more sources

BET Bromodomain Inhibitors Suppress Inflammatory Activation of Gingival Fibroblasts and Epithelial Cells From Periodontitis Patients

Frontiers in Immunology, 2019
BET bromodomain proteins are important epigenetic regulators of gene expression that bind acetylated histone tails and regulate the formation of acetylation-dependent chromatin complexes.
Anna Maksylewicz, Agnieszka Bysiek, Katarzyna B. Lagosz, Justyna M. Macina, Malgorzata Kantorowicz, Grzegorz Bereta, Maja Sochalska, Katarzyna Gawron, Maria Chomyszyn-Gajewska, Jan Potempa, Jan Potempa, Aleksander M. Grabiec   +11 more
doaj   +1 more source

Inhibition of BET Proteins and Histone Deacetylase (HDACs): Crossing Roads in Cancer Therapy. [PDF]

Cancers (Basel), 2019
Histone DeACetylases (HDACs) are enzymes that remove acetyl groups from histones and other proteins, regulating the expression of target genes. Pharmacological inhibition of these enzymes re-shapes chromatin acetylation status, confusing boundaries ...
Manzotti G, Ciarrocchi A, Sancisi V.
europepmc   +2 more sources