Results 61 to 70 of about 37,262 (190)

Dihydropyridine Lactam Analogs Targeting BET Bromodomains

ChemMedChem, 2021
AbstractInhibitors of Bromodomain and Extra Terminal (BET) proteins are investigated for various therapeutic indications, but selectivity for BRD2, BRD3, BRD4, BRDT and their respective tandem bromodomains BD1 and BD2 remains suboptimal. Here we report selectivity‐focused structural modifications of previously reported dihydropyridine lactam 6 by ...
Jiewei Jiang, Logan H. Sigua, Alice Chan, Prakriti Kalra, William C.K. Pomerantz, Ernst Schönbrunn, Jun Qi, Gunda I. Georg   +7 more
openaire   +4 more sources

1,3,4-oxadiazoles as inhibitors of the atypical member of the BET family bromodomain factor 3 from Trypanosoma cruzi (TcBDF3)

Frontiers in Microbiology
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi, affects millions globally, with increasing urban cases outside of Latin America. Treatment is based on two compounds, namely, benznidazole (BZ) and nifurtimox, but chronic cases pose ...
Victoria L. Alonso, Victoria L. Alonso, Andrea M. Escalante, Elvio Rodríguez Araya, Elvio Rodríguez Araya, Gianfranco Frattini, Gianfranco Frattini, Luis E. Tavernelli, Diego M. Moreno, Diego M. Moreno, Ricardo L. E. Furlan, Esteban Serra, Esteban Serra   +12 more
doaj   +1 more source

Pharmacologic Targeting of Chromatin Modulators As Therapeutics of Acute Myeloid Leukemia

Frontiers in Oncology, 2017
Acute myeloid leukemia (AML), a common hematological cancer of myeloid lineage cells, generally exhibits poor prognosis in the clinic and demands new treatment options.
Rui Lu, Rui Lu, Gang Greg Wang, Gang Greg Wang   +3 more
doaj   +1 more source

Super-enhancers and the super-enhancer reader BRD4: tumorigenic factors and therapeutic targets

Cell Death Discovery, 2023
Transcriptional super-enhancers and the BET bromodomain protein BRD4 are emerging as critical drivers of tumorigenesis and therapeutic targets. Characterized by substantial accumulation of histone H3 lysine 27 acetylation (H3K27ac) signals at the loci of
Haihong Qian, Min Zhu, Xinyu Tan, Yixing Zhang, Xiangning Liu, Li Yang   +5 more
doaj   +1 more source

Binding hotspots of BAZ2B bromodomain: Histone interaction revealed by solution NMR driven docking. [PDF]

, 2014
Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Alessio Ciulli, Alexandre M. J. J. Bonvin, Artimo P., Best R. B., Charlop-Powers Z., Chris Abell, Cole R., Corrêa D. H., David M. Dias, de Vries S. J., Dominguez C., Fedorov O., Ferguson F. M., Filippakopoulos P., Filippakopoulos P., Filippakopoulos P., Fleur M. Ferguson, García de la Torre J., Guetg C., Hans Wienk, Hess B., Huang D., Hwang T.-L., Jones M. H., João P. G. L. M. Rodrigues, Liu Y., Magno A., Marley J., Morris K. F., Muller S., Nicodeme E., Olsson M. H. M., Philpott M., Poplawski A., Rolf Boelens, Sun H., Trellet M., Wienk H.   +37 more
core   +6 more sources

Epigenomic regulation of heart failure: integrating histone marks, long noncoding RNAs, and chromatin architecture. [PDF]

, 2018
Epigenetic processes are known to have powerful roles in organ development across biology. It has recently been found that some of the chromatin modulatory machinery essential for proper development plays a previously unappreciated role in the ...
McKinsey, Timothy A, Vondriska, Thomas M, Wang, Yibin   +2 more
core  

Exploring the Histone Acetylation Cycle in the Protozoan Model Tetrahymena thermophila

Frontiers in Cell and Developmental Biology, 2020
The eukaryotic histone acetylation cycle is composed of three classes of proteins, histone acetyltransferases (HATs) that add acetyl groups to lysine amino acids, bromodomain (BRD) containing proteins that are one of the most characterized of several ...
Suzanne Wahab, Alejandro Saettone, Syed Nabeel-Shah, Nora Dannah, Jeffrey Fillingham   +4 more
doaj   +1 more source

Epigenetics and chromatin remodeling play a role in lung disease [PDF]

, 2011
Epigenetics is defined as heritable changes that affect gene expression without altering the DNA sequence. Epigenetic regulation of gene expression is facilitated through different mechanisms such as DNA methylation, histone modifications and RNA ...
Adcock, IM, Barnes, PJ, Masjedi, MR, Mortaz, E   +3 more
core   +1 more source

Loci specific epigenetic drug sensitivity. [PDF]

, 2020
Therapeutic targeting of epigenetic modulators offers a novel approach to the treatment of multiple diseases. The cellular consequences of chemical compounds that target epigenetic regulators (epi-drugs) are complex.
Pilko, Anna, Wollman, Roy, Zhang, Thanutra   +2 more
core   +1 more source

Blastic plasmacytoid dendritic cell neoplasm: Genomics mark epigenetic dysregulation as a primary therapeutic target [PDF]

, 2019
Blastic plasmacytoid dendritic cell neoplasm (BPDCN) is a rare and aggressive hematologic malignancy for which there is still no effective B therapy.
Abate F., Agostinelli C., Amente S., Berti E., Bertolini F., Brundu F., Cerroni L., Dellino G. I., Etebari M., Facchetti F., Falini B., Fuligni F., Indio V., Laginestra M. A., Melle F., Motta G., Orecchioni S., Paulli M., Piccioni R., Pileri A., Pileri S. A., Pimpinelli N., Rabadan R., Rossi M., Sabattini E., Sapienza M. R., Tabanelli V., Talarico G., Tarantino G., Tripodo C., Truni M.   +30 more
core   +2 more sources