A chemical probe toolbox for dissecting the cancer epigenome

Jake Shortt, Christopher J. Ott, Ricky W. Johnstone, James E. Bradner

Research output: Contribution to journalReview ArticleResearchpeer-review

57 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)160-183
Number of pages24
JournalNature Reviews Cancer
Volume17
Issue number3
DOIs
Publication statusPublished - 1 Mar 2017

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