Results 21 to 30 of about 33,428 (239)

Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy

Signal Transduction and Targeted Therapy, 2023
BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer treatment.
Zhi-Qiang Wang, Zhaocong Zhang, Yu-yang Wu, Yanan Pi, Sheng Lou, T. Liu, Ge Lou, Chang Yang   +7 more
semanticscholar   +1 more source

Distinct layers of BRD4-PTEFb reveal bromodomain-independent function in transcriptional regulation

Molecules and Cells, 2023
The BET family protein BRD4, which forms the CDK9-containing BRD4-PTEFb complex, is considered to be a master regulator of RNA Polymerase II (Pol II) pause release.
B. Zheng, Sarah Gold, Marta Iwanaszko, B. Howard, Lu Wang, A. Shilatifard   +5 more
semanticscholar   +1 more source

A Nutrient-Based Cellular Model to Characterize Acetylation-Dependent Protein-Protein Interactions

Frontiers in Molecular Biosciences, 2022
Cellular homeostasis requires the orderly expression of thousands of transcripts. Gene expression is regulated by numerous proteins that recognize post-translational modifications—in particular, the acetylation of lysine residues (Kac) on histones.
Jérémy Loehr, Jérémy Loehr, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Pata-Eting Kougnassoukou Tchara, Kevin Gonthier, Kevin Gonthier, Chahinez Noufi, Chahinez Noufi, Naomie Linteau, Naomie Linteau, Étienne Audet-Walsh, Étienne Audet-Walsh, Jean-Philippe Lambert, Jean-Philippe Lambert, Jean-Philippe Lambert   +15 more
doaj   +1 more source

Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

Journal of Medicinal Chemistry, 2021
Bromodomain and extraterminal (BET) proteins bind acetylated lysine residues in histones and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics, cellular processes, and disease procession.
Pan Tang, Jifa Zhang, Jie Liu, C. Chiang, Ouyang Liang   +4 more
semanticscholar   +1 more source

The Functions of BET Proteins in Gene Transcription of Biology and Diseases

Frontiers in Molecular Biosciences, 2021
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional regulators in biology.
Ka Lung Cheung, Claudia Kim, Ming-Ming Zhou   +2 more
doaj   +1 more source

Bromodomains as therapeutic targets [PDF]

Expert Reviews in Molecular Medicine, 2011
Acetylation of lysine residues is a post-translational modification with broad relevance to cellular signalling and disease biology. Enzymes that ‘write’ (histone acetyltransferases, HATs) and ‘erase’ (histone deacetylases, HDACs) acetylation sites are an area of extensive research in current drug development, but very few potent inhibitors that ...
Muller, S, Filippakopoulos, P, Knapp, S
openaire   +3 more sources

Discovery, X‑ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site

Journal of Medicinal Chemistry, 2022
Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 family members has stalled the collective understanding of this critical system and ...
Zhiqing Liu, Yi Li, Haiying Chen, Hsien-Tsung Lai, Pingyuan Wang, Shwu-Yuan Wu, E. Wold, P. Leonard, S. Joseph, Haitao Hu, C. Chiang, A. Brasier, B. Tian, Jia Zhou   +13 more
semanticscholar   +1 more source

Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader

, 2021
Targeted protein degradation is a powerful induced-proximity tool to control cellular concentrations of native proteins using small molecules. However, the design of selectivity in protein degradation remains challenging.
Huda, Zahid, Dan, Harki, Anand, Divakaran, Taosheng, Chen, Wenwei , Lin, william, pomerantz   +5 more
core   +1 more source

The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation

Translational Neuroscience, 2023
Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in the blood – brain barrier, brain parenchyma inflammation, and a decline of cognitive function ...
Wasiak Sylwia, Fu Li, Daze Emily, Gilham Dean, Rakai Brooke D., Stotz Stephanie C., Tsujikawa Laura M., Sarsons Chris D., Studer Deborah, Rinker Kristina D., Jahagirdar Ravi, Wong Norman C. W., Sweeney Michael, Johansson Jan O., Kulikowski Ewelina   +14 more
doaj   +1 more source

The bromodomain a chromatin browser

Frontiers in Bioscience, 2001
Reversible modification of histone tails is a regulatory step in chromatin remodeling. The N-terminal tails of histones are signaling platforms that carry amino acid residues for post-translational modification and contribute to chromosomal higher order structure. These modifications are performed by a number of chromatin modulators such as histone (h)
FILETICI P., ORNAGHI P., BALLARIO, Paola
openaire   +7 more sources