Results 91 to 100 of about 33,428 (239)

Phase 1 Study of Molibresib (GSK525762), a Bromodomain and Extra-Terminal Domain Protein Inhibitor, in NUT Carcinoma and Other Solid Tumors

JNCI Cancer Spectrum, 2019
Background Bromodomain and extra-terminal domain proteins are promising epigenetic anticancer drug targets. This first-in-human study evaluated the safety, recommended phase II dose, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity ...
S. Piha-Paul, C. Hann, C. French, S. Cousin, I. Braña, P. Cassier, V. Moreno, J. D. de Bono, Sara Harward, G. Ferron-Brady, O. Barbash, Anastasia Wyce, Yuehui Wu, Thierry Horner, Meg Annan, N. Parr, R. Prinjha, C. Carpenter, J. Hilton, D. Hong, N. Haas, M. Markowski, A. Dhar, P. O'dwyer, G. Shapiro   +24 more
semanticscholar   +1 more source

Exploring the Histone Acetylation Cycle in the Protozoan Model Tetrahymena thermophila

Frontiers in Cell and Developmental Biology, 2020
The eukaryotic histone acetylation cycle is composed of three classes of proteins, histone acetyltransferases (HATs) that add acetyl groups to lysine amino acids, bromodomain (BRD) containing proteins that are one of the most characterized of several ...
Suzanne Wahab, Alejandro Saettone, Syed Nabeel-Shah, Nora Dannah, Jeffrey Fillingham   +4 more
doaj   +1 more source

Bromodomain-containing protein BRPF1 is a therapeutic target for liver cancer

Communications Biology, 2021
Epigenetic deregulation plays an essential role in hepatocellular carcinoma (HCC) progression. Bromodomains are epigenetic “readers” of histone acetylation.
Carol Cheng, Felice Ho‐Ching Tsang, Lai Wei, Mengnuo Chen, Don Wai-Ching Chin, Jialing Shen, Cheuk-Ting Law, Derek Lee, C. C. Wong, I. Ng, Chun‐Ming Wong   +10 more
semanticscholar   +1 more source

Structural variation of protein-ligand complexes of the first bromodomain of BRD4

, 2021
The bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extra-terminal domain (BET) family, plays a key role in several diseases, especially cancers.
Ellen, Guest, Guest, Ellen E., Stephen, Pickett, Pickett, Stephen D., Jonathan, Hirst, Hirst, Jonathan D.   +5 more
core   +1 more source

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

ACS Medicinal Chemistry Letters, 2020
Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family of proteins.
Alex Preston, Stephen J. Atkinson, Paul Bamborough, Chun-wa Chung, Laurie J. Gordon, Paola Grandi, James R. J. Gray, Lee A. Harrison, Antonia J. Lewis, David Lugo, Cassie Messenger, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Inmaculada Rioja, Jon Seal, Simon Taylor, Pierre Thesmar, Ian D. Wall, Robert J. Watson, James M. Woolven, Emmanuel H. Demont   +21 more
openaire   +3 more sources

Discovery of Highly Potent BET Inhibitors based on a Tractable Tricyclic Scaffold

The bromodomain and extra-terminal domain (BET) protein family is a class of epigenetic reader proteins that recognize N-acetylated lysine residues in histone tails, playing a crucial role in gene expression and cell transcription.
Zaidi, Jaffer M., Stocks, Michael J., Chan, Weng C., Comeo, Eleonora, Baxter, Andrew, Preston, Alex G.S.   +5 more
core   +1 more source

Multivalent nucleosome scaffolding by bromodomain and extraterminal domain tandem bromodomains

Journal of Biological Chemistry
Promoter-promoter and enhancer-promoter interactions are enriched in histone acetylation and central to chromatin organization in active genetic regions. Bromodomains are epigenetic "readers" that recognize and bind histone acetylation. Bromodomains often exist in tandem or with other reader domains.
Michael D. Olp, Karina L. Bursch, Sarah L. Wynia-Smith, Raymundo Nuñez, Christopher J. Goetz, Vaughn Jackson, Brian C. Smith   +6 more
openaire   +2 more sources

Bromodomain-containing protein 4 knockdown promotes neuronal ferroptosis in a mouse model of subarachnoid hemorrhage

Neural Regeneration Research
Neuronal cell death is a common outcome of multiple pathophysiological processes and a key factor in neurological dysfunction after subarachnoid hemorrhage. Neuronal ferroptosis in particular plays an important role in early brain injury.
Peng Lu, Fan Zhang, Lei Yang, Yijing He, Xi Kong, Kecheng Guo, Yuke Xie, Huangfan Xie, Bingqing Xie, Yong Jiang, Jianhua Peng   +10 more
doaj   +1 more source

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]

PLoS ONE, 2016
Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori, Alessandra Pasquo, Clorinda Lori, Maria Petrosino, Roberta Chiaraluce, Cynthia Tallant, Stefan Knapp, Valerio Consalvi   +7 more
doaj   +1 more source

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

ACS Chemical Biology, 2015
The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1.
Michael Zengerle, Kwok-Ho Chan, A. Ciulli   +2 more
semanticscholar   +1 more source