Results 71 to 80 of about 33,428 (239)

Structural features and inhibitors of bromodomains [PDF]

Drug Discovery Today: Technologies, 2016
Bromodomains are conserved structural modules responsible for recognizing acetylated-lysine residues on histone tails and other transcription-associated proteins, such as transcription factors and co-factors. Owing to their important functions in the regulation of ordered gene transcription in chromatin, bromodomains of the BET family proteins have ...
Jamel, Meslamani, Steven G, Smith, Roberto, Sanchez, Ming-Ming, Zhou   +3 more
openaire   +2 more sources

Nucleosome conformation dictates the histone code

eLife
Histone post-translational modifications (PTMs) play a critical role in chromatin regulation. It has been proposed that these PTMs form localized ‘codes’ that are read by specialized regions (reader domains) in chromatin-associated proteins (CAPs) to ...
Matthew R Marunde, Harrison A Fuchs, Jonathan M Burg, Irina K Popova, Anup Vaidya, Nathan W Hall, Ellen N Weinzapfel, Matthew J Meiners, Rachel Watson, Zachary B Gillespie, Hailey F Taylor, Laylo Mukhsinova, Ugochi C Onuoha, Sarah A Howard, Katherine Novitzky, Eileen T McAnarney, Krzysztof Krajewski, Martis W Cowles, Marcus A Cheek, Zu-Wen Sun, Bryan J Venters, Michael-C Keogh, Catherine A Musselman   +22 more
doaj   +1 more source

Functional characterization of the catalytic and bromodomain of FgGCN5 in development, DON production and virulence of Fusarium graminearum

Journal of Integrative Agriculture, 2020
FgGCN5, a GCN5 homolog in Fusarium graminearum, plays a critical role in hyphal vegetative growth, asexual and sexual reproduction, deoxynivalenol (DON) biosynthesis and plant infection.
Qian-nan WANG, Pan-pan HUANG, Shan-yue ZHOU   +2 more
doaj   +1 more source

Enhancer Activity Requires CBP/P300 Bromodomain-Dependent Histone H3K27 Acetylation.

Cell Reports, 2018
Acetylation of histone H3 at lysine 27 is a well-defined marker of enhancer activity. However, the functional impact of this modification at enhancers is poorly understood.
Ryan M. Raisner, S. Kharbanda, Lingyan Jin, E. Jeng, E. Chan, M. Merchant, Peter M. Haverty, Russell Bainer, Tommy K. Cheung, D. Arnott, E. M. Flynn, F. A. Romero, Steven Magnuson, Karen E Gascoigne   +13 more
semanticscholar   +1 more source

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

Molecules and Cells, 2017
SUMMARY Processive elongation of RNA Polymerase II from a proximal promoter paused state is a rate-limiting event in human gene control. A small number of regulatory factors influence transcription elongation on a global scale. Prior research using small-
Georg E. Winter, Georg E. Winter, A. Mayer, Dennis L. Buckley, Michael A. Erb, J. Roderick, S. Vittori, Jaime M. Reyes, J. D. Iulio, Amanda L. Souza, Christopher J. Ott, Justin M. Roberts, Rhamy Zeid, Thomas G. Scott, Joshiawa Paulk, Kate Lachance, C. Olson, S. Dastjerdi, Sophie Bauer, Charles Y. Lin, N. Gray, M. Kelliher, L. Churchman, J. Bradner, J. Bradner   +24 more
semanticscholar   +1 more source

Fragment-Based Identification of Ligands for Bromodomain-Containing Factor 3 of Trypanosoma Cruzi

, 2020
The Trypanosoma cruzi (T. cruzi) parasite is the cause of Chagas disease, a neglected disease endemic in South America. The life cycle of the T. cruzi parasite is complex and includes transitions between distinct life stages.
Andrew, Boczek, Philip, Biggin, Stuart, Conway, Amy, Scorah, Corentine, Laurin, David, Hewings, Laura, Jennings, Fern, Woodhouse, Anthony, Chan, Philip, Humphreys, Joseph, Bluck, K. F. Larissa, See, Michelle, Keller, Matthias, Schiedel   +13 more
core   +1 more source

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
openaire   +2 more sources

Development of a Novel Positron Emission Tomography (PET) Radiotracer Targeting Bromodomain and Extra-Terminal Domain (BET) Family Proteins

Frontiers in Molecular Biosciences, 2020
Bromodomain and extra-terminal domain (BET) family proteins have become a hot research area because of their close relationship with a variety of human diseases.
Ping Bai, Ping Bai, Ping Bai, Yu Lan, Hao Wang, Zude Chen, Stephanie Fiedler, Robin Striar, Xiaoxia Lu, Changning Wang   +9 more
doaj   +1 more source

Bromodomain-containing Proteins BRD1, BRD2, and BRD13 are Core Subunits of SWI/SNF Complexes and are Vital for their Genomic Targeting in Arabidopsis.

Molecular Plant, 2021
Switch defective/sucrose non-fermentable (SWI/SNF) chromatin remodeling complexes are multi-subunit machines that play vital roles in regulating chromatin structure and gene expression.
Yaoguang Yu, Wei Fu, Jianqu Xu, Y. Lei, Xin Song, Zhenwei Liang, Tao Zhu, Yu Liang, Yuanhao Hao, Liangbing Yuan, Chenlong Li   +10 more
semanticscholar   +1 more source

Enhanced efficacy of combined temozolomide and bromodomain inhibitor therapy for gliomas using targeted nanoparticles

Nature Communications, 2018
Effective treatment for glioblastoma (GBM) is limited by the presence of the blood–brain barrier (BBB) and rapid resistance to single agent therapies.
F. Lam, Stephen W. Morton, J. Wyckoff, Tu-Lan Vu Han, Mun Kyung Hwang, Amanda Maffa, Elena Balkanska-Sinclair, M. Yaffe, S. Floyd, P. Hammond   +9 more
semanticscholar   +1 more source