A chemical probe toolbox for dissecting the cancer epigenome.

Nat Rev Cancer
Authors
Keywords
Abstract

Cancer cell hallmarks are underpinned by transcriptional programmes operating in the context of a dynamic and complicit epigenomic environment. Somatic alterations of chromatin modifiers are among the most prevalent cancer perturbations. There is a pressing need for targeted chemical probes to dissect these complex, interconnected gene regulatory circuits. Validated chemical probes empower mechanistic research while providing the pharmacological proof of concept that is required to translate drug-like derivatives into therapy for cancer patients. In this Review, we describe chemical probe development for epigenomic effector proteins that are linked to cancer pathogenesis. By annotating these reagents, we aim to share our perspectives on an informative 'epigenomic toolbox' of broad utility to the research community.

Year of Publication
2017
Journal
Nat Rev Cancer
Volume
17
Issue
3
Pages
160-183
Date Published
2017 Feb 23
ISSN
1474-1768
DOI
10.1038/nrc.2016.148
PubMed ID
28228643
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