Results 11 to 20 of about 4,858 (185)

Bromodomain Proteins in HIV Infection

Viruses, 2013
Bromodomains are conserved protein modules of ~110 amino acids that bind acetylated lysine residues in histone and non-histone proteins. Bromodomains are present in many chromatin-associated transcriptional regulators and have been linked to diverse ...
Melanie Ott, Daniela Boehm, Ryan J. Conrad   +2 more
doaj   +6 more sources

Multivalent nucleosome scaffolding by bromodomain and extraterminal domain tandem bromodomains. [PDF]

J Biol Chem
Promoter-promoter and enhancer-promoter interactions are enriched in histone acetylation and central to chromatin organization in active genetic regions. Bromodomains are epigenetic "readers" that recognize and bind histone acetylation. Bromodomains often exist in tandem or with other reader domains.
Olp MD, Bursch KL, Wynia-Smith SL, Nuñez R, Goetz CJ, Jackson V, Smith BC.   +6 more
europepmc   +3 more sources

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

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

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

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. Here, we report the successful screening of a library of nearly 1500 small molecules by high-throughput ...
Spiliotopoulos, Dimitrios, Wamhoff, Eike-Christian, Lolli, Graziano, Rademacher, Christoph, Caflisch, Amedeo   +4 more
openaire   +5 more sources

Spotlight on Plant Bromodomain Proteins

Biology, 2023
Bromodomain-containing proteins (BRD-proteins) are the “readers” of histone lysine acetylation, translating chromatin state into gene expression. They act alone or as components of larger complexes and exhibit diverse functions to regulate gene expression; they participate in chromatin remodeling complexes, mediate histone modifications, serve as ...
Eirini Bardani, Paraskevi Kallemi, Martha Tselika, Konstantina Katsarou, Kriton Kalantidis   +4 more
openaire   +3 more sources

SAR by Space: Enriching Hit Sets from the Chemical Space

Molecules, 2019
We introduce SAR by Space, a concept to drastically accelerate structure-activity relationship (SAR) elucidation by synthesizing neighboring compounds that originate from vast chemical spaces.
Franca-Maria Klingler, Marcus Gastreich, Oleksandr O. Grygorenko, Olena Savych, Petro Borysko, Anastasia Griniukova, Kateryna E. Gubina, Christian Lemmen, Yurii S. Moroz   +8 more
doaj   +1 more source

CREBBP/EP300 bromodomains are critical to sustain the GATA1/MYC regulatory axis in proliferation

Epigenetics & Chromatin, 2018
Background The reported antitumor activity of the BET family bromodomain inhibitors has prompted the development of inhibitors against other bromodomains.
Veronica Garcia-Carpizo, Sergio Ruiz-Llorente, Jacinto Sarmentero, Osvaldo Graña-Castro, David G. Pisano, Maria J. Barrero   +5 more
doaj   +1 more source

The Functions of BET Proteins in Gene Transcription of Biology and Diseases

Frontiers in Molecular Biosciences, 2021
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional regulators in biology.
Ka Lung Cheung, Claudia Kim, Ming-Ming Zhou   +2 more
doaj   +1 more source