Journal article
A chemical probe toolbox for dissecting the cancer epigenome
J Shortt, CJ Ott, RW Johnstone, JE Bradner
Nature Reviews Cancer | Published : 2017
DOI: 10.1038/nrc.2016.148
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..
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Awarded by National Institutes of Health
Funding Acknowledgements
R.W J. is funded by project and programme grants from the National Health and Medical Research Council of Australia (NHMRC), an NHMRC Senior Principal Research Fellowship and grants from the Cancer Council Victoria and the Victorian Cancer Agency (VCA). C.J.O. is supported by a Fellow Award from the Leukemia and Lymphoma Society (5667-13) and by a US National Cancer Institute (NCI) Pathway to Independence Award (K99CA190861). J.S. is supported by a Fellowship from the Eva & Les Erdi Snowdome Foundation/VCA and project grants from the Cancer Council of Victoria and NHMRC. J.E.B. is supported by research grants from the US National Institutes of Health (NIH) (R01-CA176745 and P01-CA066996), the William Lawrence & Blanche Hughes Foundation and a Leukemia & Lymphoma Society Specialized Center of Research (SCOR) grant.