Results 21 to 30 of about 4,858 (185)

Discovery of the natural product 3',4',7,8-tetrahydroxyflavone as a novel and potent selective BRD4 bromodomain 2 inhibitor

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Bromodomain-containing protein 4 (BRD4) binds acetylated lysine residues on the N-terminal tails of histones through two bromodomains (BD1 and BD2) to regulate gene transcription.
Jiao Li, Wei Zou, Koukou Yu, Bing Liu, Weifeng Liang, Lisha Wang, Yin Lu, Zequn Jiang, Aiyun Wang, Jiapeng Zhu   +9 more
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Bromodomain biology and drug discovery [PDF]

Nature Structural & Molecular Biology, 2019
The bromodomain (BrD) is a conserved structural module found in chromatin- and transcription-associated proteins that acts as the primary reader for acetylated lysine residues. This basic activity endows BrD proteins with versatile functions in the regulation of protein-protein interactions mediating chromatin-templated gene transcription, DNA ...
Nilesh Zaware, Ming-Ming Zhou
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A bromodomain–DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT

Nature Communications, 2016
Many chromatin modifying proteins, including BRDT, contain bromodomains, which are known to interact with nucleosomes. Here, the authors find that BRDT interacts with nucleosomes via only one of its two bromodomains, and that the interaction involves ...
Thomas C. R. Miller, Bernd Simon, Vladimir Rybin, Helga Grötsch, Sandrine Curtet, Saadi Khochbin, Teresa Carlomagno, Christoph W. Müller   +7 more
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Accurate absolute free energies for ligand–protein binding based on non-equilibrium approaches

Communications Chemistry, 2021
Molecular dynamics-based approaches to calculate absolute protein–ligand binding free energy often rely on equilibrium free energy perturbation (FEP) protocols.
Vytautas Gapsys, Ahmet Yildirim, Matteo Aldeghi, Yuriy Khalak, David van der Spoel, Bert L. de Groot   +5 more
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Selective inhibition of BET bromodomains [PDF]

Nature, 2010
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described.
Filippakopoulos, P, Qi, J, Picaud, S, Shen, Y, Smith, W, Fedorov, O, Morse, E, Keates, T, Hickman, T, Felletar, I, Philpott, M, Munro, S, McKeown, M, Wang, Y, Christie, A, West, N, Cameron, M, Schwartz, B, Heightman, T, La Thangue, N, French, C, Wiest, O, Kung, A, Knapp, S, Bradner, J   +24 more
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Discovery of a Novel Aminocyclopropenone Compound That Inhibits BRD4-Driven Nucleoporin NUP210 Expression and Attenuates Colorectal Cancer Growth

Cells, 2022
Epigenetic deregulation plays an essential role in colorectal cancer progression. Bromodomains are epigenetic “readers” of histone acetylation. Bromodomain-containing protein 4 (BRD4) plays a pivotal role in transcriptional regulation and is a feasible ...
Hiroya Kondo, Kenji Mishiro, Yuki Iwashima, Yujia Qiu, Akiko Kobayashi, Keesiang Lim, Takahiro Domoto, Toshinari Minamoto, Kazuma Ogawa, Munetaka Kunishima, Masaharu Hazawa, Richard W. Wong   +11 more
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Methylpyrrole inhibitors of BET bromodomains [PDF]

Bioorganic & Medicinal Chemistry Letters, 2017
An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced ...
Lisa A, Hasvold, George S, Sheppard, Le, Wang, Steven D, Fidanze, Dachun, Liu, John K, Pratt, Robert A, Mantei, Carol K, Wada, Robbert, Hubbard, Yu, Shen, Xiaoyu, Lin, Xiaoli, Huang, Scott E, Warder, Denise, Wilcox, Leiming, Li, F Greg, Buchanan, Lauren, Smithee, Daniel H, Albert, Terrance J, Magoc, Chang H, Park, Andrew M, Petros, Sanjay C, Panchal, Chaohong, Sun, Peter, Kovar, Nirupama B, Soni, Steven W, Elmore, Warren M, Kati, Keith F, McDaniel   +27 more
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Bdf1 Bromodomains Are Essential for Meiosis and the Expression of Meiotic-Specific Genes.

PLoS Genetics, 2017
Bromodomain and Extra-terminal motif (BET) proteins play a central role in transcription regulation and chromatin signalling pathways. They are present in unicellular eukaryotes and in this study, the role of the BET protein Bdf1 has been explored in ...
Encar García-Oliver, Claire Ramus, Jonathan Perot, Marie Arlotto, Morgane Champleboux, Flore Mietton, Christophe Battail, Anne Boland, Jean-François Deleuze, Myriam Ferro, Yohann Couté, Jérôme Govin   +11 more
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Brd4’s Bromodomains Mediate Histone H3 Acetylation and Chromatin Remodeling in Pluripotent Cells through P300 and Brg1

Cell Reports, 2018
Summary: The pluripotent state of embryonic stem cells (ESCs) is defined by its transcriptome and epigenome. The chromatin reader Brd4 determines ESC identity.
Tao Wu, Yasunao F. Kamikawa, Mary E. Donohoe   +2 more
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Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities

Molecules, 2023
Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid.
Maria Karelou, Dionysis Kampasis, Amalia D. Kalampaliki, Leentje Persoons, Andreas Krämer, Dominique Schols, Stefan Knapp, Steven De Jonghe, Ioannis K. Kostakis   +8 more
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