Results 191 to 200 of about 33,428 (239)

Butyrate blocks specific histone acetylation by preventing recruitment of p300 to acetylated histones

Jiang M, Psoma A, Lyu J, Chiariello MG, Modderman R, Bianchi F, Incarnato D, Marrink S, Jonkers IH, van den Bogaart G.   +9 more
europepmc   +1 more source

Discovery of BAZ2A bromodomain ligands [PDF]

European Journal of Medicinal Chemistry, 2017
The bromodomain adjacent to zinc finger domain protein 2A (BAZ2A) is implicated in aggressive prostate cancer. The BAZ2A bromodomain is a challenging target because of the shallow pocket of its natural ligand, the acetylated side chain of lysine.
Eike-Christian Wamhoff, Graziano Lolli, Christoph Rademacher   +2 more
exaly   +9 more sources

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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.
M. Schwalm, S. Knapp
semanticscholar   +3 more sources

Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases.

Journal of Medicinal Chemistry, 2023
Selective inhibitors targeting the first bromodomain (BD1) or the second bromodomain (BD2) of the bromodomain and extra terminal domain (BET) proteins have triggered extensive research to produce more specific agents.
Zhijie Wang, Lingfeng Yin, Zhenghan Xiong, Fei Huang, Na Yang, Fei Jiang, Huili Li, Yong Cui, Jiwei Ren, Zitian Cheng, Kun Jia, Tao Lu, Jiapeng Zhu, Qinghua Hu, Yadong Chen   +14 more
semanticscholar   +1 more source

Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.

Journal of Medicinal Chemistry, 2022
Blocking the interactions between bromodomain and extraterminal (BET) proteins and acetylated lysines of histones by small molecules has important implications for the treatment of cancers and other diseases.
Juncheng Chen, Pan Tang, Yuxi Wang, Jiaxing Wang, Chengcan Yang, Yang Li, Gaoxia Yang, Fengbo Wu, Jifa Zhang, Ouyang Liang   +9 more
semanticscholar   +1 more source

Bromodomain and extraterminal domain protein bromodomain inhibitor based cancer therapeutics

Current Opinion in Oncology, 2021
Purpose of review Bromodomain and extraterminal domain (BET) proteins are evolutionarily conserved, multifunctional super-regulators that specifically recognize acetyl-lysine on histones and other proteins controlling gene transcription.
Tithi Ghosh, Halder, Raffaella, Soldi, Sunil, Sharma   +2 more
openaire   +2 more sources

Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.

Journal of Medicinal Chemistry, 2022
ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While several small molecule inhibitors have been described in the literature, their cellular activity has ...
J. Winter-Holt, C. Bardelle, E. Chiarparin, I. Dale, Paul R. J. Davey, Nichola L. Davies, C. Denz, Shaun M. Fillery, Carine M Guérot, Fujin Han, S. Hughes, M. Kulkarni, Zhaoqun Liu, A. Milbradt, T. Moss, H. Niu, J. Patel, A. Rabow, M. Schimpl, Junjie Shi, Dongqing Sun, Dejian Yang, S. Guichard   +22 more
semanticscholar   +1 more source

Bromodomains and Their Pharmacological Inhibitors

ChemMedChem, 2014
AbstractOver 60 bromodomains belonging to proteins with very different functions have been identified in humans. Several of them interact with acetylated lysine residues, leading to the recruitment and stabilization of protein complexes. The bromodomain and extra‐terminal domain (BET) proteins contain tandem bromodomains which bind to acetylated ...
Daniel, Gallenkamp, Kathy A, Gelato, Bernard, Haendler, Hilmar, Weinmann   +3 more
openaire   +2 more sources

Discovery of N-ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET bromodomain inhibitor with selectivity for the second bromodomain.

Journal of Medicinal Chemistry, 2020
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under clinical development for oncology bind to each of the eight bromodomains with ...
G. Sheppard, Le Wang, S. Fidanze, Lisa A. Hasvold, Dachun Liu, J. Pratt, Chang H. Park, K. Longenecker, W. Qiu, M. Torrent, P. Kovar, M. Bui, Emily J. Faivre, Xiaoli Huang, Xiaoyu Lin, Denise M. Wilcox, Lu Zhang, Yu Shen, D. Albert, T. Magoc, G. Rajaraman, W. Kati, K. McDaniel   +22 more
semanticscholar   +1 more source

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.

Journal of Medicinal Chemistry, 2022
Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery efforts.
Alexander M. Taylor, C. Bailey, L. Belmont, R. Campbell, N. Cantone, A. Côté, Terry D Crawford, R. Cummings, Kevin DeMent, M. Duplessis, M. Flynn, A. Good, Hon-Ren Huang, Shivangi Joshi, Y. Leblanc, J. Murray, C. Nasveschuk, A. Neiss, F. Poy, F. A. Romero, P. Sandy, Yong Tang, V. Tsui, L. Zawadzke, R. Sims, J. Audia, S. Bellon, Steven Magnuson, B. Albrecht, A. Cochran   +29 more
semanticscholar   +1 more source