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Epigenomes 2018, 2(3), 16; https://doi.org/10.3390/epigenomes2030016

Targeting EZH2 in Multiple Myeloma—Multifaceted Anti-Tumor Activity

1
Division of Hematology and Oncology, Department of Medicine, University of Florida Health Cancer Center, University of Florida, Gainesville, FL 32610, USA
2
Science for Life Laboratory, Department of Immunology, Genetics and Pathology, Rudbeck Laboratory, Uppsala University, Uppsala, SE-75185 Uppsala, Sweden
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 8 August 2018 / Revised: 29 August 2018 / Accepted: 29 August 2018 / Published: 3 September 2018
(This article belongs to the Special Issue Polycomb and Trithorax Group of Proteins in Development and Disease)
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Abstract

The enhancer of zeste homolog 2 (EZH2) is the enzymatic subunit of the polycomb repressive complex 2 (PRC2) that exerts important functions during normal development as well as disease. PRC2 through EZH2 tri-methylates histone H3 lysine tail residue 27 (H3K27me3), a modification associated with repression of gene expression programs related to stem cell self-renewal, cell cycle, cell differentiation, and cellular transformation. EZH2 is deregulated and subjected to gain of function or loss of function mutations, and hence functions as an oncogene or tumor suppressor gene in a context-dependent manner. The development of highly selective inhibitors against the histone methyltransferase activity of EZH2 has also contributed to insight into the role of EZH2 and PRC2 in tumorigenesis, and their potential as therapeutic targets in cancer. EZH2 can function as an oncogene in multiple myeloma (MM) by repressing tumor suppressor genes that control apoptosis, cell cycle control and adhesion properties. Taken together these findings have raised the possibility that EZH2 inhibitors could be a useful therapeutic modality in MM alone or in combination with other targeted agents in MM. Therefore, we review the current knowledge on the regulation of EZH2 and its biological impact in MM, the anti-myeloma activity of EZH2 inhibitors and their potential as a targeted therapy in MM. View Full-Text
Keywords: epigenetics; EZH2; multiple myeloma; epigenetic therapy epigenetics; EZH2; multiple myeloma; epigenetic therapy
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Alzrigat, M.; Jernberg-Wiklund, H.; Licht, J.D. Targeting EZH2 in Multiple Myeloma—Multifaceted Anti-Tumor Activity. Epigenomes 2018, 2, 16.

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