Bromodomains as therapeutic targets

S Muller, P Filippakopoulos, S Knapp - Expert reviews in molecular …, 2011 - cambridge.org
Acetylation of lysine residues is a post-translational modification with broad relevance to
cellular signalling and disease biology. Enzymes that 'write'(histone acetyltransferases …

[HTML][HTML] The bromodomain interaction module

P Filippakopoulos, S Knapp - FEBS letters, 2012 - Elsevier
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 …

Histone recognition and large-scale structural analysis of the human bromodomain family

P Filippakopoulos, S Picaud, M Mangos, T Keates… - Cell, 2012 - cell.com
Bromodomains (BRDs) are protein interaction modules that specifically recognize ε-N-lysine
acetylation motifs, a key event in the reading process of epigenetic marks. The 61 BRDs in …

Suppression of inflammation by a synthetic histone mimic

E Nicodeme, KL Jeffrey, U Schaefer, S Beinke… - Nature, 2010 - nature.com
Interaction of pathogens with cells of the immune system results in activation of inflammatory
gene expression. This response, although vital for immune defence, is frequently deleterious …

Discovery and characterization of small molecule inhibitors of the BET family bromodomains

C Chung, H Coste, JH White, O Mirguet… - Journal of medicinal …, 2011 - ACS Publications
Epigenetic mechanisms of gene regulation have a profound role in normal development and
disease processes. An integral part of this mechanism occurs through lysine acetylation of …

[HTML][HTML] The role of human bromodomains in chromatin biology and gene transcription

R Sanchez, MM Zhou - Current opinion in drug discovery & …, 2009 - ncbi.nlm.nih.gov
The acetylation of histone lysine is central to providing the dynamic regulation of chromatin-
based gene transcription. The bromodomain (BRD), which is the conserved structural …

Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical …

A Chaidos, V Caputo… - Therapeutic advances in …, 2015 - journals.sagepub.com
Post-translational modifications of the nucleosomal histone proteins orchestrate chromatin
organization and gene expression in normal and cancer cells. Among them, the acetylation …

Double bromodomain‐containing gene Brd2 is essential for embryonic development in mouse

E Shang, X Wang, D Wen, DA Greenberg… - Developmental …, 2009 - Wiley Online Library
Double bromodomain‐containing gene Brd2 is essential for embryonic development in mouse -
Shang - 2009 - Developmental Dynamics - Wiley Online Library Skip to Article Content Skip to …

Bromo-and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration

SS Gupta, T Maetzig, GN Maertens, A Sharif… - Journal of …, 2013 - Am Soc Microbiol
Retroviral integrase (IN) proteins catalyze the permanent integration of proviral genomes
into host DNA with the help of cellular cofactors. Lens epithelium-derived growth factor …

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

M Philpott, J Yang, T Tumber, O Fedorov… - Molecular …, 2011 - pubs.rsc.org
Histone lysine acetylation is a key component of epigenetic regulation of gene transcription.
Bromodomains, found in histone acetyl transferases and other chromatin-associated …