Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas Review


Authors: Morschhauser, F.; Salles, G.; Batlevi, C. L.; Tilly, H.; Chaidos, A.; Phillips, T.; Burke, J.; Melnick, A.
Review Title: Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas
Abstract: Enhancer of zeste homolog 2 (EZH2) is an epigenetic regulator that controls the normal biology of germinal B cells. Overexpression or mutation of EZH2 is associated with malignant transformation in a number of B-cell malignancies; thus, EZH2 inhibitors are an attractive therapeutic option for these targets. Several EZH2 inhibitors have entered clinical trials, but there remains an important question as to how EZH2 inhibitor mechanism of action differs in patients with mutant and wild-type EZH2. This review discusses the EZH2-driven mechanisms that lead to the development of B-cell lymphomas and act as therapeutic targets. Another key area of investigation is whether EZH2 inhibitors will work synergistically with existing immunomodulatory drugs and chemotherapy regimens. In summary, EZH2 inhibitors show potential as treatment for a range of B-cell lymphomas, and numerous clinical evaluations are currently underway. © 2022 The Authors
Keywords: lymphoma; b cell; epigenomics; tazemetostat; ezh2 inhibitor
Journal Title: Blood Reviews
Volume: 56
ISSN: 0268-960X
Publisher: Churchill Livingstone  
Date Published: 2022-11-01
Start Page: 100988
Language: English
DOI: 10.1016/j.blre.2022.100988
PUBMED: 35851487
PROVIDER: scopus
DOI/URL:
Notes: Review -- Export Date: 1 November 2022 -- Source: Scopus
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  1. Connie Wing-Ching Lee Batlevi
    176 Batlevi
  2. Gilles Andre Salles
    272 Salles