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Targeting components of epigenome by small molecules

Archives of Pharmacal Research volume 37, pages 1367–1374 (2014)Cite this article

Abstract

The diverse epigenetic modifications regulate the gene expression and determine the cellular identity. Pioneering work over the past decades has highlighted that these epigenetic regulations establish normal development but also contribute various diseases. Furthermore, the epigenetic priming events are considered as a key factor for efficient master transcription factor(s) mediated reprogramming process. With the advent of numerous small molecules that target specific enzymes or proteins involved in the epigenetic regulation of gene expression, the utilization of epigenetic targets is emerging as a valuable approach to cancer therapy and cellular reprogramming. Here, we briefly present the basic principles of epigenetic regulations and review the recent application of epigenetic targeting small molecules.

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Acknowledgments

This work was supported by the faculty research fund of Konkuk University in 2013. We would like to thank Jessica Charlet for helpful discussion and careful reading of the manuscript.

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  1. Insitute of Biomedical Science & Technology, Departments of Biochemistry, School of Medicine, Konkuk University, Seoul, Korea

    Jueng Soo You

  2. Research Center for Epigenome Regulation, Department of Biochemistry and Molecular Biology, School of Pharmacy, Sungkyunkwan University, Suwon, Korea

    Jeong Hwan Han

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You, J.S., Han, J.H. Targeting components of epigenome by small molecules. Arch. Pharm. Res. 37, 1367–1374 (2014). https://doi.org/10.1007/s12272-014-0455-9

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  • DOI: https://doi.org/10.1007/s12272-014-0455-9

Keywords

  • Small molecules
  • Epigenome
  • Cancer
  • Cellular reprogramming