Results 81 to 90 of about 33,428 (239)

Molecular Basis for the N‑Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase–Bromodomain Inhibitor

, 2018
As regulators of transcription, epigenetic proteins that interpret post-translational modifications to N-terminal histone tails are essential for maintaining cellular homeostasis. When dysregulated, “reader” proteins become drivers of disease.
John C. Widen (1951051), Joseph J. Topczewski (1323912), William C. K. Pomerantz (1476328), Jin-Yi Zhu (1319226), Ernst K. Schonbrunn (5858630), Anand Divakaran (2041456), Norbert Berndt (1319235), Daniel A. Harki (1523884), Neeraj K. Mishra (1507708), Huarui Cui (5858624), Siva K. Talluri (5858621), Alex M. Ayoub (4092883), Angela S. Carlson (5858627)   +12 more
core   +2 more sources

BET Bromodomain Inhibitor iBET151 Impedes Human ILC2 Activation and Prevents Experimental Allergic Lung Inflammation

Frontiers in Immunology, 2019
Group 2 innate lymphoid cells (ILC2) increase in frequency in eczema and allergic asthma patients, and thus represent a new therapeutic target cell for type-2 immune-mediated disease.
Bernhard Kerscher, Jillian L. Barlow, Batika M. Rana, Helen E. Jolin, Mayuri Gogoi, Michelle A. Bartholomew, Deepali Jhamb, Ashutosh Pandey, David F. Tough, Antoon J. M. van Oosterhout, Andrew N. J. McKenzie   +10 more
doaj   +1 more source

Chemical Inhibition of Bromodomain Proteins in Insect-Stage African Trypanosomes Perturbs Silencing of the Variant Surface Glycoprotein Repertoire and Results in Widespread Changes in the Transcriptome

Microbiology Spectrum, 2023
The eukaryotic protozoan parasite Trypanosoma brucei is transmitted by the tsetse fly to both humans and animals, where it causes a fatal disease called African trypanosomiasis.
Ethan C. Ashby, Jennifer L. Havens, Lindsey M. Rollosson, Johanna Hardin, Danae Schulz   +4 more
doaj   +1 more source

Dynamic chromatin: concerted nucleosome remodelling and acetylation [PDF]

, 2005
The flexibility of chromatin that enables translation of environmental cues into changes in genome utilisation, relies on a battery of enzymes able to modulate chromatin structure in a highly targeted and regulated manner.
Eberharter, Anton, Becker, Peter, Ferreira, Roger   +2 more
core   +1 more source

Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma

eLife, 2016
Pharmacological inhibition of chromatin co-regulatory factors represents a clinically validated strategy to modulate oncogenic signaling through selective attenuation of gene expression.
Andrew R Conery, Richard C Centore, Adrianne Neiss, Patricia J Keller, Shivangi Joshi, Kerry L Spillane, Peter Sandy, Charlie Hatton, Eneida Pardo, Laura Zawadzke, Archana Bommi-Reddy, Karen E Gascoigne, Barbara M Bryant, Jennifer A Mertz, Robert J Sims III   +14 more
doaj   +1 more source

Synthesis and Structure–Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research

Molecules, 2021
Epigenetic regulation is known to play a key role in progression of anti-cancer therapeutics. Lysine acetylation is an important mechanism in controlling gene expression.
Minjin Yoo, Tae Hyun Park, Miyoun Yoo, Yeongrin Kim, Joo-Youn Lee, Kyu Myung Lee, Seong Eon Ryu, Byung Il Lee, Kwan-Young Jung, Chi Hoon Park   +9 more
doaj   +1 more source

Bromodomain proteins regulate human cytomegalovirus latency and reactivation allowing epigenetic therapeutic intervention

Proceedings of the National Academy of Sciences of the United States of America, 2021
Significance Human cytomegalovirus (HCMV) reactivation is a major cause of posttransplant morbidity/mortality. One approach toward reducing this is purging the transplant donor and/or recipient of latently infected cells prior to stem-cell or organ ...
Ian J. Groves, Sarah E. Jackson, Emma Poole, A. Nachshon, Batsheva Rozman, M. Schwartz, R. Prinjha, D. Tough, J. Sinclair, M. Wills   +9 more
semanticscholar   +1 more source

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