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Accepted (AM)Open Access (License Unspecified), Open
Journal article
Live-Cell Studies of p300/CBP Histone Acetyltransferase Activity and Inhibition
Chembiochem : a European journal of chemical biology, v 13(14), pp 2113-2121
24 Sep 2012
PMID: 22961914
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
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.
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Details
- Title
- Live-Cell Studies of p300/CBP Histone Acetyltransferase Activity and Inhibition
- Creators
- Beverley M. Dancy - Johns Hopkins UniversityNicholas T. Crump - University of OxfordDaniel J. Peterson - Kennedy Krieger InstituteChandrani Mukherjee - Johns Hopkins UniversityErin M. Bowers - Johns Hopkins UniversityYoung-Hoon Ahn - Johns Hopkins UniversityMinoru Yoshida - RIKENJin Zhang - Johns Hopkins UniversityLouis C. Mahadevan - University of OxfordDavid J. Meyers - Johns Hopkins MedicineJef D. Boeke - Johns Hopkins MedicinePhilip A. Cole - Johns Hopkins Medicine
- Publication Details
- Chembiochem : a European journal of chemical biology, v 13(14), pp 2113-2121
- Publisher
- Wiley
- Number of pages
- 9
- Grant note
- U54RR020839 / NATIONAL CENTER FOR RESEARCH RESOURCES; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Center for Research Resources (NCRR) R01DK073368 / NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of Diabetes & Digestive & Kidney Diseases (NIDDK) R01GM062437 / NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute of General Medical Sciences (NIGMS) U54-RR020839; GM62437; R01-DK073368 / National Institutes of Health; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- College of Arts and Sciences; Chemistry; Drexel University
- Web of Science ID
- WOS:000308933300015
- Scopus ID
- 2-s2.0-84866465308
- Other Identifier
- 991020100071304721
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- Collaboration types
- Domestic collaboration
- International collaboration
- Web of Science research areas
- Biochemistry & Molecular Biology
- Chemistry, Medicinal