
Therapeutic targeting of EP300/CBP by bromodomain inhibition in ...
Nov 22, 2023 · EP300 and CREBBP are paralogous genes coding for multi-domain acetyltransferases targeting diverse proteins. 1,2,3 EP300/CBP is an attractive therapeutic target in cancer due to its roles in promoting growth and transformation.
Bromodomain inhibition of the coactivators CBP/EP300 ... - Nature
Apr 8, 2019 · Here, we identify acetyl-lysine competitive inhibitors targeting the bromodomains of coactivators CREB (cyclic-AMP response element binding protein) binding protein (CBP) and E1A binding protein of...
HDAC8-mediated inhibition of EP300 drives a transcriptional
Nov 29, 2023 · Using ATAC-Seq and ChIP-Seq we show that increased HDAC8 activity alters chromatin structure by increasing H3K27ac and enhancing accessibility at c-Jun binding sites. Functionally, HDAC8...
EP300 Selectively Controls the Enhancer Landscape of
Mar 1, 2022 · Chromatin immunoprecipitation coupled to high-throughput sequencing (ChIP-seq) studies have identified largely overlapping but distinct binding of EP300 and CBP genome-wide, indicating that these two proteins may function differently by …
Analysis and therapeutic targeting of the EP300 and CREBBP ...
Dec 1, 2022 · In the current study, we investigated the physiological roles of EP300 and CREBBP in both ALCL and HL, and exploited the therapeutic potential of EP300/CREBBP small molecule inhibitors that...
EP300/CREBBP acetyltransferase inhibition limits steroid receptor …
Apr 4, 2024 · The ChIP-seq analyses confirmed that EP300 binds to the GRBs (Supplementary Fig. S6 e and S7c), and this binding is significantly enhanced by Dex-treatment, especially in ENZ-treated 22Rv1 cells.
Mapping cell type-specific transcriptional enhancers using high ...
Cre recombinase-directed, cell type specific expression of BirA, an E. coli enzyme that biotinylates the bio epitope tag (de Boer et al., 2003), allows selective Ep300 ChIP-seq, thereby identifying enhancers active in the cell type of interest.
CCS1477 (inobrodib) is a potent, selective EP300/CBP bromodomain inhibitor which induces cell-cycle ar-rest and differentiation in hematologic malignancy model systems.
Integration of ChIP-seq and machine learning reveals enhancers …
Feb 17, 2012 · We employ ChIP-seq for EP300 and H3K4me1 to identify melanocyte enhancers genome-wide. We use a novel set of criteria that takes into account both EP300 and H3K4me1 to define a single set of putative enhancers, and validate these enhancers through a series of in silico, in vitro, and in vivo analyses.
Ep300 sequestration to functionally distinct glucocorticoid …
Jul 7, 2022 · Ep300 chromatin immunoprecipitation (ChIP) assay and sequencing 3134 cells were cultured in CSS for 24 h and treated with either vehicle (EtOH) or 100 nM Dex for 1 h.