Dynamics of sequestering the limiting p300/CBP, viral cis-regulatory elements, and disease
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Biosciences"
DOI: 10.1007/s12038-020-00051-4
Abstract: Many studies showed that the p300/CBP coactivator is limiting. Here we review three studies that showed how transcription complexes formed on viral cis-regulator elements compete with cellular transcription complexes by sequestrating the p300/CBP coactivator. According… read more here.
Keywords: cis; disease; cis regulatory; viral cis ... See more keywords
A novel histone acetyltransferase inhibitor A485 improves sensitivity of non-small-cell lung carcinoma cells to TRAIL.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical pharmacology"
DOI: 10.1016/j.bcp.2020.113914
Abstract: Transcriptional coactivators p300 and CBP catalyze the acetylation of lysine residues in histone proteins. Upregulation of p300 and CBP has been associated with lung, colorectal and hepatocellular cancer, indicating an important role of p300 and… read more here.
Keywords: non small; cell; inhibitor a485; p300 cbp ... See more keywords
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00670
Abstract: E1A binding protein (p300) and CREB binding protein (CBP) are two highly homologous and multidomain histone acetyltransferases. These two proteins are involved in many cellular processes by acting as coactivators of a large number of… read more here.
Keywords: p300; proline based; p300 cbp; inhibitors using ... See more keywords
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00096
Abstract: Herein, we report the discovery of a series of new P300/CBP-associated factor (PCAF) bromodomain (BRD) inhibitors, which were obtained through a hit discovery process and subsequent structure-based optimization and structure-activity relationship analyses toward a retrieved… read more here.
Keywords: discovery; cbp associated; associated factor; p300 cbp ... See more keywords
P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib.
Sign Up to like & getrecommendations! Published in 2021 at "Acta pharmacologica Sinica"
DOI: 10.1038/s41401-021-00643-2
Abstract: Mantle cell lymphoma (MCL) is a lymphoproliferative disorder lacking reliable therapies. PI3K pathway contributes to the pathogenesis of MCL, serving as a potential target. However, idelalisib, an FDA-approved drug targeting PI3Kδ, has shown intrinsic resistance… read more here.
Keywords: mcl; idelalisib; inhibition; p300 cbp ... See more keywords
Glucose derived carbon nanosphere (CSP) conjugated TTK21, an activator of the histone acetyltransferases CBP/p300, ameliorates amyloid‐beta 1–42 induced deficits in plasticity and associativity in hippocampal CA1 pyramidal neurons
Sign Up to like & getrecommendations! Published in 2022 at "Aging Cell"
DOI: 10.1111/acel.13675
Abstract: The master epigenetic regulator lysine acetyltransferase (KAT) p300/CBP plays a pivotal role in neuroplasticity and cognitive functions. Recent evidence has shown that in several neurodegenerative diseases, including Alzheimer's disease (AD), the expression level and function… read more here.
Keywords: ttk21; p300 cbp; carbon nanosphere; p300 ... See more keywords
p300/CBP as a Key Nutritional Sensor for Hepatic Energy Homeostasis and Liver Fibrosis
Sign Up to like & getrecommendations! Published in 2018 at "BioMed Research International"
DOI: 10.1155/2018/8168791
Abstract: The overwhelming frequency of metabolic diseases such as obesity and diabetes are closely related to liver diseases, which might share common pathogenic signaling processes. These metabolic disorders in the presence of inflammatory response seem to… read more here.
Keywords: energy homeostasis; liver fibrosis; p300 cbp; liver ... See more keywords
Abstract 1020: p300 and CBP targeting in castration therapy resistant prostate cancer
Sign Up to like & getrecommendations! Published in 2019 at "Endocrinology"
DOI: 10.1158/1538-7445.am2019-1020
Abstract: p300 and CBP interact with transcription factors and other proteins via their histone acetyltransferase domain (HAT) and a bromodomain (Bd). In prostate cancer, p300 and CBP act as oncogenes and are commonly upregulated. p300 and… read more here.
Keywords: prostate cancer; p300 cbp; cbp; enza ... See more keywords
Abstract A091: Therapeutic targeting of the p300/CBP bromodomain for the treatment of castration-resistant prostate cancer
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.prca2017-a091
Abstract: Background: Sustained androgen receptor pathway activation is the hallmark of castration-resistant prostate cancer (CRPC). Therapeutic strategies for CRPC include non-ligand-binding domain targeted degradation of androgen receptor (AR) and AR variants (ARV). E1A binding protein (p300)… read more here.
Keywords: cancer; castration resistant; p300 cbp; p300 ... See more keywords
The p300 and CBP Transcriptional Coactivators Are Required for β-Cell and α-Cell Proliferation
Sign Up to like & getrecommendations! Published in 2017 at "Diabetes"
DOI: 10.2337/db17-0237
Abstract: p300 (EP300) and CBP (CREBBP) are transcriptional coactivators with histone acetyltransferase activity. Various β-cell transcription factors can recruit p300/CBP, and thus the coactivators could be important for β-cell function and health in vivo. We hypothesized… read more here.
Keywords: cell; transcriptional coactivators; p300 cbp; proliferation ... See more keywords
New Inhibitors of the Human p300/CBP Acetyltransferase Are Selectively Active against the Arabidopsis HAC Proteins
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms231810446
Abstract: Histone acetyltransferases (HATs) are involved in the epigenetic positive control of gene expression in eukaryotes. CREB-binding proteins (CBP)/p300, a subfamily of highly conserved HATs, have been shown to function as acetylases on both histones and… read more here.
Keywords: inhibitors human; human p300; hac; p300 cbp ... See more keywords