Frontiers in Endocrinology, 2022 Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D).
Joshua A. Nord +8 more
doaj +1 more source
Bromodomains: pockets with therapeutic potential
Trends in Molecular Medicine, 2014 Intense interest in the complex biology of the bromodomain (BRD) protein modules has fueled the development of novel small molecule inhibitors that target the acetyl-lysine (KAc) binding pocket of the BRD. BRD inhibition has revealed exciting opportunities for treating a variety of maladies such as cancer, inflammation, obesity, cardiovascular disease,
Papavassiliou, Kostas A. +1 more
openaire +3 more sources
Theoretical Studies of Several Small-Ring Precursors to (+)-JQ1 [PDF]
, 2013 We present the results of DFT(B3LYP) calculations on several precursors to (+)-JQ1 using an accurate basis set, including a report of conformational analysis, thermochemistry, optimized geometries and electrostatic potentials, and calculated IR and Raman
Atkinson, Elizabeth J. O. +2 more
core +1 more source
Chemical synthesis of the ATAD2 bromodomain [PDF]
Proceedings of the National Academy of Sciences, 2014 Significance The bromodomain–histone binding motif has been shown to read epigenetic marks on chromatin, and proteins with a bromodomain can have powerful effects on gene expression and transcriptional regulation. ATAD2 is one such protein and has been linked to a wide variety of cancers with expression of ATAD2 correlating strongly with a ...
Gardner S, Creech +3 more
openaire +2 more sources
Is now the time for molecular driven therapy for diffuse large B-cell lymphoma? [PDF]
, 2017 INTRODUCTION: Recent genetic and molecular discoveries regarding alterations in diffuse large B-cell lymphoma (DLBCL) deeply changed the approach to this lymphoproliferative disorder.
Ansuinelli, Michela +4 more
core +1 more source
Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains [PDF]
, 2018 Bromodomains have been pursued intensively over the past several years as emerging targets for the development of anticancer and anti-inflammatory agents.
Alessi, Dario R. +27 more
core +3 more sources
Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development [PDF]
, 2017 Parasitic infections remain one of the most pressing global health concerns of our day, affecting billions of people and producing unsustainable economic burdens.
Huang, Sherri +3 more
core +1 more source
Advanced ScienceThe fungal Bromodomain and Extra‐Terminal (BET) protein Bdf1 is a potential antifungal target against invasive fungal infections. However, the need to selectively inhibit both Bdf1 bromodomains (BDs) over human orthologs and the lack of molecular tools ...
Kaiyao Wei +22 more
doaj +1 more source
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology [PDF]
, 2016 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, the readers of acetyl-lysine modifications.
Alessio Ciulli +3 more
core +2 more sources
Central role of Yes-associated protein and WW-domain-containing transcriptional co-activator with PDZ-binding motif in pancreatic cancer development. [PDF]
, 2019 Pancreatic ductal adenocarcinoma (PDAC) remains a deadly disease with no efficacious treatment options. PDAC incidence is projected to increase, which may be caused at least partially by the obesity epidemic.
Eibl, Guido, Rozengurt, Enrique
core