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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 ...
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 ...
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 ...
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 ...
Trypanosoma cruzi bromodomain factor 2 (BDF2) binds to acetylated histones and is accumulated after UV irradiation
(Elsevier B.V., 2009-05-01)
Histone tail post-translational modifications (acetylation, methylation, phosphorylation, ubiquitination and ADP-ribosylation) regulate many cellular processes. Among these modifications, phosphorylation, methylation and ...
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 ...
Design and synthesis of hybrid compounds as epigenetic modifiers
(2021-12-01)
Epigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains ...
Trypanosoma cruzi Bromodomain Factor 3 Binds Acetylated α-Tubulin and Concentrates in the Flagellum during Metacyclogenesis
(American Society For Microbiology, 2014-04)
Bromodomains are highly conserved acetyl-lysine binding domains found mainly in proteins associated with chromatin and nuclear acetyltransferases. The Trypanosoma cruzi genome encodes at least four bromodomain factors ...