Results 21 to 30 of about 27,094 (219)

Binding hotspots of BAZ2B bromodomain:histone interaction revealed by solution NMR driven docking [PDF]

, 2014
Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Ferguson, Fleur M., Alexandre M. J. J. Bonvin (18079), Alexandre M. J. J. Bonvin, João P. G. L. M. Rodrigues (1312506), Wienk, Hans, Fleur M. Ferguson (1304613), Rolf Boelens (18078), Alessio Ciulli, Boelens, Rolf, NMR Spectroscopy, Chris Abell, Fleur M. Ferguson, Garcia Lopes Maia Rodrigues, João, Rodrigues, João P. G. L. M., David M. Dias, Bonvin, Alexandre M. J. J., Sub NMR Spectroscopy, Dias, David M., João P. G. L. M. Rodrigues, David M. Dias (1340694), Rolf Boelens, Abell, Chris, Hans Wienk (684663), Ciulli, Alessio, Hans Wienk, Chris Abell (197099), Alessio Ciulli (762789)   +26 more
core   +3 more sources

TP53 R249S mutation in hepatic organoids captures the predisposing cancer risk

Hepatology, EarlyView., 2022
The systematic approach in elucidating the gain‐of‐function (GOF) roles of TP53 mutations in early liver carcinogenesis. Unique downstream targets of TP53 L3 mutations were identified from chormatin immunoprecipitation sequencing in HCC cell lines, followed by a series of validation assays to substantiate the exclusive transcriptional regulations ...
Yin Kau Lam, Jianqing Yu, Hao Huang, Xiaofan Ding, Alissa M. Wong, Howard H. Leung, Anthony W. Chan, Kelvin K. Ng, Mingjing Xu, Xin Wang, Nathalie Wong   +10 more
wiley   +1 more source

Hydrophobic Waters in Bromodomains [PDF]

The 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery, 2019
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains due to their implication in cancer, inflammation, and a plethora of diseases.
Serena G. Piticchio, Miriam Martínez-Cartró, Salvatore Scaffidi, Sergio Rodríguez-Arévalo, Andrea Bagán, Ainoa Sánchez-Arfelis, Carmen Escolano, Carles Galdeano, Xavier Barril   +8 more
openaire   +3 more sources

Rational design and development of selective BRD7 bromodomain inhibitors and their activity in prostate cancer [PDF]

, 2023
Bromodomain-containing proteins are readers of acetylated lysine and play important roles in cancer. Bromo-domain-containing protein 7 (BRD7) has been implicated in multiple malignancies; however, there are no selective chemical probes to study its ...
Sandra, Ordonez, Surbhi, Sood, Alexander, McQuade, Brian , Smith, Sijie, Wang, Emily, Dykhuizen, Brayden, Strohmier, Chad, Maschinot   +7 more
core   +2 more sources

Tumor-Promoting ATAD2 and Its Preclinical Challenges

Biomolecules, 2022
ATAD2 has received extensive attention in recent years as one prospective oncogene with tumor-promoting features in many malignancies. ATAD2 is a highly conserved bromodomain family protein that exerts its biological functions by mainly AAA ATPase and ...
Haicheng Liu, Qianghai Wen, Sheng Yan, Weikun Zeng, Yuhua Zou, Quanliang Liu, Guoxi Zhang, Junrong Zou, Xiaofeng Zou   +8 more
doaj   +1 more source

Bromodomains as therapeutic targets [PDF]

Expert Reviews in Molecular Medicine, 2011
Acetylation of lysine residues is a post-translational modification with broad relevance to cellular signalling and disease biology. Enzymes that ‘write’ (histone acetyltransferases, HATs) and ‘erase’ (histone deacetylases, HDACs) acetylation sites are an area of extensive research in current drug development, but very few potent inhibitors that ...
Muller, S, Filippakopoulos, P, Knapp, S
openaire   +3 more sources

Developing inhibitors of bromodomain-histone interactions [PDF]

, 2014
Lysine acetylation is a widespread protein post-translational modification that influences diverse cellular processes. An association between acetylation of histone N-terminal tails and transcriptional activation has been recognised since the 1960s ...
Hewings, David Stephen, Conway, Stuart J, Brennan, Paul E   +2 more
core   +2 more sources

The bromodomain interaction module [PDF]

FEBS Letters, 2012
ε‐N‐acetylation of lysine residues (Kac) is one of the most abundant post‐translation modifications (PTMs) in the human proteome. In the nucleus, acetylation of histones has been linked to transcriptional activation of genes but the functional consequences of most acetylation events and proteins recruited to these sites remains largely unknown ...
Filippakopoulos, P, Knapp, S
openaire   +2 more sources

Identification of a BAZ2A-Bromodomain Hit Compound by Fragment Growing [PDF]

, 2022
BAZ2A is an epigenetic regulator affecting transcription of ribosomal RNA. It is overexpressed in aggressive and recurrent prostate cancer, promoting cellular migration. Its bromodomain is characterized by a shallow and difficult-to-drug pocket. Here, we
Spiliotopoulos, Dimitrios, Corsi, Jessica, Cazzanelli, Giulia, Caflisch, Amedeo; https://orcid.org/, Batiste, Laurent, Dalle Vedove, Andrea, Marchand, Jean-Rémy; https://orcid.org/, D'Agostino, Vito Giuseppe, Lolli, Graziano; https://orcid.org/   +8 more
core   +1 more source

Bioactivation of Isoxazole-Containing Bromodomain and Extra-Terminal Domain (BET) Inhibitors

Metabolites, 2021
The 3,5-dimethylisoxazole motif has become a useful and popular acetyl-lysine mimic employed in isoxazole-containing bromodomain and extra-terminal (BET) inhibitors but may introduce the potential for bioactivations into toxic reactive metabolites.
Noah R. Flynn, Michael D. Ward, Mary A. Schleiff, Corentine M. C. Laurin, Rohit Farmer, Stuart J. Conway, Gunnar Boysen, S. Joshua Swamidass, Grover P. Miller   +8 more
doaj   +1 more source