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Getting a handle on chemical probes of chomatin readers.

Authors
  • Waybright, Jarod M1, 2
  • James, Lindsey I1, 2
  • 1 Center for Integrative Chemical Biology & Drug Discovery, Division of Chemical Biology & Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • 2 UNC Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Type
Published Article
Journal
Future Medicinal Chemistry
Publisher
"Future Science, LTD"
Publication Date
Apr 01, 2021
Volume
13
Issue
8
Pages
749–763
Identifiers
DOI: 10.4155/fmc-2019-0274
PMID: 31920100
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

The dynamic nature of histone post-translational modifications such as methylation or acetylation makes possible the alteration of disease associated epigenetic states through the manipulation of the associated epigenetic machinery. One approach is through small molecule perturbation. Chemical probes of epigenetic reader domains have been critical in improving our understanding of the biological consequences of modulating their targets, while also enabling the development of novel probe-based reagents. By appending a functional handle to a reader domain probe, a chemical toolbox of reagents can be created to facilitate chemiprecipitation of epigenetic complexes, evaluate probe selectivity, develop in vitro screening assays, visualize cellular target localization, enable target degradation and recruit epigenetic machinery to a site within the genome in a highly controlled fashion.

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