Results 251 to 260 of about 24,956 (275)

BET bromodomain inhibitors

Current Opinion in Chemical Biology, 2022
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P Schwalm, Stefan Knapp
exaly   +3 more sources

Development of methyl isoxazoleazepines as inhibitors of BET

Bioorganic and Medicinal Chemistry Letters, 2015
In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified by carboxamide 23. The methyl isoxazoleazepine chemotype provides potent inhibition of the bromodomains of the BET family ...
Michael C Hewitt, Alexandre Coté, Eneída Pardo   +2 more
exaly   +3 more sources

Quercetin Enhances the Anti-Tumor Effects of BET Inhibitors by Suppressing hnRNPA1

International Journal of Molecular Sciences, 2019
Bromodomain and extraterminal domain (BET) proteins, which are important epigenetic readers, are often dysregulated in cancer. While a number of BET inhibitors are currently in early phase clinical trials, BET inhibitors show limited single-agent ...
Thao N D Pham, Mario A Shields, Christina Spaulding   +2 more
exaly   +2 more sources

BET bromodomain inhibitors in leukemia

Experimental Hematology, 2015
The last few years have seen the identification of bromodomain and extraterminal (BET) proteins as critical mediators of transcription with effects on its direct control and cisregulation. This discovery is important in furthering our understanding of the mechanisms of normal transcriptional control. Subsequent work has shed light on the multiple roles
Faisal, Basheer, Brian J P, Huntly
openaire   +2 more sources

Increasing the saturation of BET inhibitors

, 2018
Previously held under moratorium in Chemistry department (GSK) from 6 June 2018 until 18 June 2021The confidentiality statement on each page of this thesis DOES NOT applyBromodomains are epigenetic reader modules that are found as part of multidomain ...
Dixon, Joseph Edward
openaire   +3 more sources

BET Inhibition-Induced GSK3β Feedback Enhances Lymphoma Vulnerability to PI3K Inhibitors

Cell Reports, 2018
The phosphatidylinositol 3 kinase (PI3K)-glycogen synthase kinase β (GSK3β) axis plays a central role in MYC-driven lymphomagenesis, and MYC targeting with bromodomain and extraterminal protein family inhibitors (BETi) is a promising treatment strategy ...
Enrico Derenzini, Patrizia Mondello, Tatiana Erazo   +2 more
exaly   +2 more sources

Physachenolide C is a Potent, Selective BET Inhibitor

Journal of Medicinal Chemistry, 2022
A pulldown using a biotinylated natural product of interest in the 17β-hydroxywithanolide (17-BHW) class, physachenolide C (PCC), identified the bromodomain and extra-terminal domain (BET) family of proteins (BRD2, BRD3, and BRD4), readers of acetyl-lysine modifications and regulators of gene transcription, as potential cellular targets.
Christopher J. Zerio, Jared Sivinski, E. M. Kithsiri Wijeratne, Ya-Ming Xu, Duc T. Ngo, Andrew J. Ambrose, Luis Villa-Celis, Niloofar Ghadirian, Michael W. Clarkson, Donna D. Zhang, Nancy C. Horton, A. A. Leslie Gunatilaka, Raimund Fromme, Eli Chapman   +13 more
openaire   +2 more sources

BET bromodomain inhibitors regulate keratinocyte plasticity

Nature Chemical Biology, 2021
Although most acute skin wounds heal rapidly, non-healing skin ulcers represent an increasing and substantial unmet medical need that urgently requires effective therapeutics. Keratinocytes resurface wounds to re-establish the epidermal barrier by transitioning to an activated, migratory state, but this ability is lost in dysfunctional chronic wounds ...
Gabi Schutzius, Christian Kolter, Sebastian Bergling, Federico Tortelli, Florian Fuchs, Steffen Renner, Vito Guagnano, Simona Cotesta, Heinrich Rueeger, Michael Faller, Laure Bouchez, Adrian Salathe, Florian Nigsch, Shola M. Richards, Malvina Louis, Viktoria Gruber, Alexandra Aebi, Jonathan Turner, Frederic Grandjean, Jun Li, Chris Dimitri, Jason R. Thomas, Markus Schirle, Jutta Blank, Peter Drueckes, Andrea Vaupel, Ralph Tiedt, Paul W. Manley, Julia Klopp, Rene Hemmig, Florence Zink, Nelly Leroy, Walter Carbone, Guglielmo Roma, Caroline Gubser Keller, Natalie Dales, Armin Beyerbach, Alfred Zimmerlin, Debora Bonenfant, Remi Terranova, Amy Berwick, Sukhdeep Sahambi, Aimee Reynolds, Lori L. Jennings, Heinz Ruffner, Peter Tarsa, Tewis Bouwmeester, Vickie Driver, Mathias Frederiksen, Felix Lohmann, Susan Kirkland   +50 more
openaire   +2 more sources

BET bromodomain inhibitors: a patent review

Expert Opinion on Therapeutic Patents, 2013
The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT). These "epigenetic readers" bind to acetyllysine (KAc) residues on the tails of histones H3 and H4, and regulate chromatin structure and gene expression.
Jean-Marc, Garnier, Phillip P, Sharp, Christopher J, Burns   +2 more
openaire   +2 more sources

BET Inhibitors as Anticancer Agents: A Patent Review

Recent Patents on Anti-Cancer Drug Discovery, 2017
Bromodomain and Extra Terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery.This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related ...
Imran, Ali, Gildon, Choi, Kwangho, Lee
openaire   +2 more sources