Histone acetyltransferase enzymes (HATs) are important therapeutic targets, but there are few cell-based assays available for evaluating the pharmacodynamics of HAT inhibitors. Here we present the application of a FRET-based reporter, Histac, in live-cell studies of p300/CBP HAT inhibition, by both genetic and pharmacologic disruption. shRNA knockdown of p300/CBP led to increased Histac FRET, thus suggesting a role for p300/CBP in the acetylation of the histone H4 tail. Additionally, we describe a new p300/CBP HAT inhibitor, C107, and show that it can also increase cellular Histac FRET. Taken together, these studies provide a live-cell strategy for identifying and evaluating p300/CBP inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3517098 | PMC |
| http://dx.doi.org/10.1002/cbic.201200381 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Investigating the delivery of PD-L1-targeted immunoliposomes in a dynamic cervical cancer-on-a-chip model.
J Control Release
January 2025
Precision Medicine in Oncology (PrMiO), and Nanomedicine Innovation Center Erasmus (NICE), Department of Pathology, Erasmus MC Cancer Institute, Erasmus MC, Dr. Molewaterplein 40, 3015 GD Rotterdam, the Netherlands. Electronic address:
The recent approval of pembrolizumab in recurrent or metastatic cervical cancer warrants further investigations into the usefulness of immunotherapies for more durable and less radical interventions. In this study, the targeting potential of anti-PD-L1-functionalized immunoliposomes was tested in a 3D in vitro cervical cancer-on-a-chip model. Immunolipsomes were synthesized and decorated externally with monovalent anti-PD-L1 Fab' fragments of commercially available atezolizumab.
View Article and Find Full Text PDFDifferential Mitochondrial Redox Responses to the Inhibition of NAD Salvage Pathway of Triple Negative Breast Cancer Cells.
Cancers (Basel)
December 2024
Britton Chance Laboratory of Redox Imaging, Department of Radiology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA.
: Cancer cells rely on metabolic reprogramming that is supported by altered mitochondrial redox status and an increased demand for NAD. Over expression of Nampt, the rate-limiting enzyme of the NAD biosynthesis salvage pathway, is common in breast cancer cells, and more so in triple negative breast cancer (TNBC) cells. Targeting the salvage pathway has been pursued for cancer therapy.
View Article and Find Full Text PDFCellular Response of Immune Cells in the Upper Respiratory Tract After Treatment with Cold Atmospheric Plasma In Vitro.
Int J Mol Sci
December 2024
Department of Dermatology, University Medical Center Regensburg, 93053 Regensburg, Germany.
Cold atmospheric plasma (CAP) has antimicrobial properties and is also known to stimulate the immune system. These properties could be useful for the development of a novel therapeutic or preventive strategy against respiratory infections in the upper respiratory tract (URT) such as ventilator-associated pneumonia (VAP) without inducing an immune overreaction. This study investigated the cellular responses of polymorphonuclear neutrophils (PMNs) after exposure to CAP in a three-dimensional (3D) model of the URT.
View Article and Find Full Text PDFSystematic Evaluation of Extracellular Coating Matrix on the Differentiation of Human-Induced Pluripotent Stem Cells to Cortical Neurons.
Int J Mol Sci
December 2024
Shenzhen Key Laboratory of Neuroimmunomodulation for Neurological Diseases, Shenzhen-Hong Kong Institute of Brain Science, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China.
Induced pluripotent stem cell (iPSC)-derived neurons (iNs) have been widely used as models of neurodevelopment and neurodegenerative diseases. Coating cell culture vessels with extracellular matrixes (ECMs) gives structural support and facilitates cell communication and differentiation, ultimately enhances neuronal functions. However, the relevance of different ECMs to the natural environment and their impact on neuronal differentiation have not been fully characterized.
View Article and Find Full Text PDFSurprising features of nuclear receptor interaction networks revealed by live-cell single-molecule imaging.
Elife
January 2025
Department of Molecular and Cell Biology, Berkeley, United States.
Type II nuclear receptors (T2NRs) require heterodimerization with a common partner, the retinoid X receptor (RXR), to bind cognate DNA recognition sites in chromatin. Based on previous biochemical and overexpression studies, binding of T2NRs to chromatin is proposed to be regulated by competition for a limiting pool of the core RXR subunit. However, this mechanism has not yet been tested for endogenous proteins in live cells.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!