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Current Hematologic Malignancy Reports
Published in: Current Hematologic Malignancy Reports 5/2018

01-10-2018 | B-cell NHL, T-cell NHL, and Hodgkin Lymphoma (J Amengual, Section Editor)

Emerging EZH2 Inhibitors and Their Application in Lymphoma

Authors: Jennifer K. Lue, Jennifer E. Amengual

Published in: Current Hematologic Malignancy Reports | Issue 5/2018

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Abstract

Purpose of Review

Enhancer of Zeste Homolog 2 (EZH2) is histone methyltransferase and catalyzes the methylation of histone 3 lysine 27, a mark of transcriptional repression. Various studies have elucidated the complex role of EZH2 in both normal biology and tumorigenesis. Here, we critically review the emerging role of EZH2 in malignancies, the development of small molecule inhibitors of EZH2, and their application in lymphoma.

Recent Findings

Activating mutations and overexpression of EZH2 are found in non-Hodgkin lymphoma (NHL). As a result, several EZH2 inhibitors have been developed and entered clinical investigation. Tazemetostat, first-in-class EZH2 inhibitor, demonstrated enhanced clinical activity in mutant follicular lymphoma and diffuse large B cell lymphoma.

Summary

With the early activity noted by tazemetostat in B cell lymphomas, the role of EZH2 inhibition in NHL is becoming more evident. This can be leveraged in future rationale combinations to enhance the activity of EZH2 inhibitors.
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Metadata
Title
Emerging EZH2 Inhibitors and Their Application in Lymphoma
Authors
Jennifer K. Lue
Jennifer E. Amengual
Publication date
01-10-2018
Publisher
Springer US
Published in
Current Hematologic Malignancy Reports / Issue 5/2018
Print ISSN: 1558-8211
Electronic ISSN: 1558-822X
DOI
https://doi.org/10.1007/s11899-018-0466-6

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