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Recent Progress in the Discovery of Epigenetic Inhibitors for the Treatment of Cancer

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Cancer Epigenetics

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1238))

Abstract

Epigenetics investigates heritable changes in gene transcription that do not involve a change in DNA sequence, and an increased understanding in the role of epigenetic misregulation as a key contributor to cancer has triggered the development of epigenetic targeted cancer therapies. Among these include efforts around a class of enzymes known as histone methyltransferases (HMTs). The level of interest in the development of HMT inhibitors as a class of anticancer agents has significantly grown beyond academic settings, and in the last 5 years whole research groups from biotech and big pharma have been dedicated to this area. There are now multiple reports describing small-molecule HMT inhibitors, including chemical probes and drug candidates entering the clinic as first-in-class agents. Recent progress in this emerging area is the topic of this chapter.

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Disclosures and Acknowledgments

The author is an employee and shareholder of GlaxoSmithKline. All studies conducted at GlaxoSmithKline (GSK) were conducted in accordance with the GSK Policy on the Care, Welfare and Treatment of Laboratory Animals and were reviewed at the Institutional Animal Care and Use Committee either at GSK or by the ethical review process at the institution where the work was performed. The author is thankful to Drs. C. Creasy, J. Luengo, and C. Carpenter for their reviews.

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Authors and Affiliations

  1. GlaxoSmithKline Pharmaceuticals, Inc., 1250 South Collegeville Road, Collegeville, PA, 19426, USA

    Sharad K. Verma

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  1. Sharad K. Verma
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Correspondence to Sharad K. Verma .

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Editors and Affiliations

  1. National Institutes of Health, Rockville, Maryland, USA

    Mukesh Verma

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Verma, S.K. (2015). Recent Progress in the Discovery of Epigenetic Inhibitors for the Treatment of Cancer. In: Verma, M. (eds) Cancer Epigenetics. Methods in Molecular Biology, vol 1238. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-1804-1_35

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  • DOI: https://doi.org/10.1007/978-1-4939-1804-1_35

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  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-1803-4

  • Online ISBN: 978-1-4939-1804-1

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