Results 131 to 140 of about 33,428 (239)

Non-canonical reader modules of BAZ1A promote recovery from DNA damage

Nature Communications, 2017
ISWI chromatin remodelers regulate DNA accessibility and have been implicated in DNA damage repair. Here, the authors uncover functions, in response to DNA damage, for the bromodomain of the ISWI subunit BAZ1B and for the non-canonical PHD and ...
Mariano Oppikofer, Meredith Sagolla, Benjamin Haley, Hui-Min Zhang, Sarah K. Kummerfeld, Jawahar Sudhamsu, E. Megan Flynn, Tianyi Bai, Jennifer Zhang, Claudio Ciferri, Andrea G. Cochran   +10 more
doaj   +1 more source

Global chemoproteomic profiling of bromodomain inhibitors

Bromodomain-containing proteins (BCPs) are epigenetic readers that regulate gene expression and play key roles in many diseases including cancer, making them prime targets for drug discovery. While several high-quality chemical probes and inhibitors have
Bauer, Ludwig Gerhard
core   +1 more source

Chemical proteomic profiling of bromodomains enables the wide-spectrum evaluation of bromodomain inhibitors in living cells

, 2019
Bromodomains, epigenetic 'readers' of lysine acetylation marks, exist in different nuclear proteins with diverse biological functions in chromatin biology.
Tian, G, Li, XD, Jiang, Y, Liu, Z, Deng, H, Meng, X, Li, X, Wu, Y, Feng, L, Bao, X, Sun, H   +10 more
core   +2 more sources

Bromodomain Protein Inhibition Protects β-Cells from Cytokine-Induced Death and Dysfunction via Antagonism of NF-κB Pathway

Cells
Cytokine-induced β-cell apoptosis is a major pathogenic mechanism in type 1 diabetes (T1D). Despite significant advances in understanding its underlying mechanisms, few drugs have been translated to protect β-cells in T1D.
Vinny Negi, Jeongkyung Lee, Varun Mandi, Joseph Danvers, Ruya Liu, Eliana M. Perez-Garcia, Feng Li, Rajaganapati Jagannathan, Ping Yang, Domenic Filingeri, Amit Kumar, Ke Ma, Mousumi Moulik, Vijay K. Yechoor   +13 more
doaj   +1 more source

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors

, 2015
Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of
Bhumika V. Karamshi (1562527), Amanda J. Emmons (1562518), Kelly Locke (1562521), Emma J. Jones (1343448), Nathalie Barrett (153158), Robert J. Watson (1503289), Emmanuel H. Demont (1399288), Rebecca C. Furze (1562512), Angela M. Bridges (1562536), Andy D. Roberts (1562530), Peter D. Craggs (1343430), Bernadette H. Mouzon (1562533), Paola Grandi (1343472), Anne-Marie Michon (1343457), Chun-wa Chung (1343454), Darren J. Mitchell (1343451), Robert J. Sheppard (1343445), Paul Bamborough (1343466), Hawa Diallo (1432720), Chris Wellaway (1562515), Rab K. Prinjha (449759), David P. Dixon (1562524), Clement Douault (1432714)   +22 more
core   +1 more source

Structure-based discovery of selective BRPF1 bromodomain inhibitors

, 2018
Bromodomain and plant homeodomain (PHD) finger containing protein 1 (BRPF1) is a member of subfamily IV of the human bromodomains. Experimental evidence suggests that BRPF1 is involved in leukemia.
Chunxian Zhou, Zhou, Chunxian, Amedeo Caflisch, Zhu, Jian, Jian Zhu, Caflisch, Amedeo   +5 more
core   +1 more source

Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization

Pharmaceuticals
Background: Bromodomain and extra-terminal (BET) proteins are critical regulators of gene transcription, as they recognize acetylated lysine residues. The BD1 bromodomain of BRD4, a member of the BET family, has emerged as a promising therapeutic target ...
Yongle Wang, Yanli Wang, Yulong Xu, Hua Cheng, Tewodros Mulugeta Dagnew, Leyi Kang, Darcy Tocci, Iris Z. Shen, Can Zhang, Changning Wang   +9 more
doaj   +1 more source

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching

, 2018
Background Acetylation of lysine residues in histone tails plays an important role in the regulation of gene transcription. Bromdomains are the readers of acetylated histone marks, and, consequently, bromodomain-containing proteins have a
Rogers, Catherine M, Gingras, Anne-Claude, Knapp, Stefan, Yapp, Clarence, Lambert, Jean-Philippe, Strain-Damerell, Claire, Müller, Susanne, Philpott, Martin, Wells, Chris, Burgess-Brown, Nicola A   +9 more
core   +1 more source

Bromodomain [PDF]

, 2020
openaire   +1 more source

Development of a Lysine-Reactive Targeted Covalent Inhibitor for the P300/CBP-Associated Factor Bromodomain Through Structure-Based Design. [PDF]

ChemMedChem
Ede RR, Peterson KE, Begyinah RK, Tom IP, Ochoada JM, Sneddon MS, Tiu AKY, Fischer M, Shelat AA, Pomerantz WCK.   +9 more
europepmc   +1 more source