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Overexpression of bromodomain factor 3 in Trypanosoma cruzi (TcBDF3) affects differentiation of the parasite and protects it against bromodomain inhibitors
(Wiley Blackwell Publishing, Inc, 2016-06)
The bromodomain is the only protein domain known to bind acetylated lysine. In the last few years many bromodomain inhibitors have been developed in order to treat diseases such as cancer caused by aberrant acetylation of ...
Aim for the readers! Bromodomains as new targets against Chagas` disease
(Bentham Science Publishers, 2018-10)
Bromodomains recognize and bind acetyl-lysine residues present in histone and non-histone proteins in a specific manner. Inthe last decade they have raised as attractive target for drug discovery because the miss-regulation ...
A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts
(American Chemical Society, 2018-04)
A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one ...
Dietary compound resveratrol is a pan-BET bromodomain inhibitor
(2017-11-01)
The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains ...
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain
(American Chemical Society - ACSWashington, DC, 2013-12)
Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower ...
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry
(American Chemical Society, 2018-10)
Target-directed dynamic combinatorial chemistry (DCC) has emerged as a strategy for the identification of inhibitors of relevant therapeutic targets. In this contribution, we use this strategy for the identification of a ...
Glycosomal bromodomain factor 1 from Trypanosoma cruzi enhances trypomastigote cell infection and intracellular amastigote growth
(Portland Press, 2015-12)
Acetylation is a ubiquitous protein modification present in prokaryotic and eukaryotic cells that participates in the regulation of many cellular processes. The bromodomain is the only domain known to bind acetylated lysine ...
HIV latency reversal agents: A potential path for functional cure?
(2021-03-05)
Despite the advances in Human Immunodeficiency Virus (HIV) treatment, the cure for all HIV patients still poses a major challenge, which needs to be surpassed in the coming years. Among the strategies pursuing this aim, ...
A comprehensive study of epigenetic alterations in hepatocellular carcinoma identifies potential therapeutic targets
(Elsevier Science, 2019-03)
Background & Aims: A causal link has recently been established between epigenetic alterations and hepatocarcinogenesis, indicating that epigenetic inhibition may have therapeutic potential. We aimed to identify and target ...
BET bromodomain inhibitors PFI-1 and JQ1 are identified in an epigenetic compound screen to enhance C9ORF72 gene expression and shown to ameliorate C9ORF72-associated pathological and behavioral abnormalities in a C9ALS/FTD model
(2021)
Abstract
Background
An intronic GGGGCC (G4C2) hexanucleotide repeat expansion (HRE) in the C9ORF72 gene is the most common cause of amyotrophic lateral sclerosis (ALS) and ...