Results 161 to 170 of about 128,101 (191)

The Bromodomain and Extra-Terminal Domain (BET) Family: Functional Anatomy of BET Paralogous Proteins

International Journal of Molecular Sciences, 2016
The Bromodomain and Extra-Terminal Domain (BET) family of proteins is characterized by the presence of two tandem bromodomains and an extra-terminal domain.
Yasushi Taniguchi
exaly   +2 more sources

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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

Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe

ACS Medicinal Chemistry Letters, 2018
Several chemical probes have been developed for use in fluorescence polarization screening assays to aid in drug discovery for the bromodomain and extra-terminal domain (BET) proteins. However, few of those have been characterized in the literature.
Jon E Hawkinson, William C K Pomerantz, Md Rezaul Karim   +2 more
exaly   +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   +3 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

Targeting BET Bromodomains for Cancer Treatment

Epigenomics, 2015
The bromodomain and extraterminal (BET) subfamily of bromodomain-containing proteins has emerged in the last few years as an exciting, novel target group. BRD4, the best studied BET protein, is implicated in a number of hematological and solid tumors. This is linked to its role in modulating transcription elongation of essential genes involved in cell ...
Marie, Jung, Kathy A, Gelato, Amaury, Fernández-Montalván, Stephan, Siegel, Bernard, Haendler   +4 more
openaire   +2 more sources

BET bromodomain inhibition suppresses adipogenesis in mice

Endocrine, 2019
We recently reported that inhibition of BET bromodomain suppresses adipogenesis in vitro. In the present study we aimed to address whether BET bromodomain inhibition can suppress adipogenesis in vivo.Brd4fl/fl mice were crossed with B6.Cg-Tg(Fabp4-cre)1Rev/J mice to generate Brd4fl/+/Fabp4-cre mice.
Tianlun Yang, Lingyan Zhu, Jun Qi
exaly   +3 more sources

Place your BETs: the therapeutic potential of bromodomains

Trends in Pharmacological Sciences, 2012
Therapeutic targeting of the processes that regulate histone modification is a growing area of scientific exploration. Although most interest has concentrated on the various families of enzymes that contribute to these processes, this review focuses on emerging data demonstrating the chemical tractability and therapeutic potential of a hitherto ...
R K, Prinjha, J, Witherington, K, Lee
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Naphthyridines as Novel BET Family Bromodomain Inhibitors

ChemMedChem, 2013
AbstractBromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including gene transcription and mRNA ...
Olivier, Mirguet, Yann, Lamotte, Chun-Wa, Chung, Paul, Bamborough, Delphine, Delannée, Anne, Bouillot, Françoise, Gellibert, Gael, Krysa, Antonia, Lewis, Jason, Witherington, Pascal, Huet, Yann, Dudit, Lionel, Trottet, Edwige, Nicodeme   +13 more
openaire   +2 more sources

Bet Bromodomains’ Functions in Bone-Related Pathologies

Epigenomics, 2019
Throughout life, bones are subjected to the so-called 'bone-remodeling' process, which is a balanced mechanism between the apposition and the resorption of bone. This remodeling process depends on the activities of bone-specialized cells, namely the osteoblasts and the osteoclasts.
Jacques, Camille, Lavaud, Melanie, Georges, Steven, Tesfaye, Robel, Baud'Huin, Marc, Lamoureux, François, Ory, Benjamin, Baud’huin, Marc   +7 more
openaire   +4 more sources