Results 41 to 50 of about 128,101 (191)
An RNAi-based dimorphic genetic screen identified the double bromodomain protein BET-1 as a sumo-dependent attenuator of RAS-mediated signalling. [PDF]
PLoS ONE, 2013 Attenuation of RAS/RAF/MAPK signalling is essential to prevent hyperactivation of this oncogenic pathway. In C. elegans, the sumoylation pathway and a combination of histone tail modifications regulate gene expression to attenuate the LET-60 (RAS ...
Fiona Gee +3 more
doaj +1 more source
BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment [PDF]
, 2017 Full list of authors omitted for brevity. For full list see article.Processive elongation of RNA Polymerase II from a proximal promoter paused state is a rate-limiting event in human gene control.
Roderick, Justine E. +3 more
core +2 more sources
Angewandte Chemie, EarlyView.BZ2 is a second‐generation Bromodomain PHD finger Transcription Factor (BPTF) inhibitor with improved selectivity over Class I and Class IV BRD off‐targets identified in our previously reported inhibitor, BZ1. Structural analyses reveal that water network engagement is key to this selectivity.
Kesavan Babu +19 more
wiley +2 more sources
TRPM3-Induced Gene Transcription Is under Epigenetic Control
Pharmaceuticals, 2022 Transient receptor potential M3 (TRPM3) cation channels regulate numerous biological functions, including gene transcription. Stimulation of TRPM3 channels with pregnenolone sulfate activates stimulus-responsive transcription factors, which bind to short
Gerald Thiel, Oliver G. Rössler
doaj +1 more source
Discovery of Highly Potent BET Inhibitors based on a Tractable Tricyclic Scaffold [PDF]
The bromodomain and extra-terminal domain (BET) protein family is a class of epigenetic reader proteins that recognize N-acetylated lysine residues in histone tails, playing a crucial role in gene expression and cell transcription.
Zaidi, Jaffer M. +5 more
core +1 more source
Archives of Medicine and Health SciencesWith an emphasis on their methods of action, preclinical data, and clinical development, this study attempts to investigate the potential of BET bromodomain inhibitors as innovative disease-modifying treatments for heart failure.
Omar Elsaka
doaj +1 more source
Data in Brief, 2016 Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on histone tails. Data presented here supports the manuscript published in Atherosclerosis “RVX-208,
Sylwia Wasiak +12 more
doaj +1 more source
Cell Reports, 2013 A hallmark of retroviral replication is integration of the viral genome into host cell DNA. This characteristic makes retrovirus-based vectors attractive delivery vehicles for gene therapy.
Jan De Rijck +11 more
doaj +1 more source
Segmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase A.
PLoS ONE, 2016 Bromodomain and extra-terminal (BET) family of proteins are one of the major readers of epigenetic marks and an important target class in oncology and other disease areas. The importance of the BET family of proteins is manifested by the explosion in the
Felix P Williams +3 more
doaj +1 more source
Targeting BET bromodomain proteins in solid tumors [PDF]
, 2017 There is increasing interest in inhibitors targeting BET (bromodomain and extra-terminal) proteins because of the association between this family of proteins and cancer progression.
Collier, Katharine A. +4 more
core +1 more source