2. Academic Validation
  3. Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas

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

  • Blood Rev. 2022 Nov:56:100988. doi: 10.1016/j.blre.2022.100988.
Franck Morschhauser 1,  Gilles Salles 2,  Connie Lee Batlevi 2,  Hervé Tilly 3,  Aristeidis Chaidos 4,  Tycel Phillips 5,  John Burke 6,  Ari Melnick 7
Affiliations

Affiliations

  • 1 Univ. Lille, CHU Lille, ULR 7365 - GRITA - Groupe de Recherche sur les formes Injectables et les Technologies Associées, F-59000 Lille, France. Electronic address: franck.morschhauser@chru-lille.fr.
  • 2 Memorial Sloan Kettering Cancer Center, New York, NY, USA.
  • 3 Department of Hematology, INSERM U1245, Centre Henri Becquerel and Rouen University, Rouen, France.
  • 4 The Hugh and Josseline Langmuir Centre for Myeloma Research, Centre for Haematology, Department of Immunology and Inflammation, Faculty of Medicine, Imperial College London & Hammersmith Hospital, Imperial College Healthcare NHS Trust, London, UK.
  • 5 Division of Hematology and Oncology, University of Michigan, Ann Arbor, MI, USA.
  • 6 US Oncology Hematology Research Program, Rocky Mountain Cancer Centers, Aurora, CO, USA.
  • 7 Weill Cornell Medicine, New York, NY, USA. Electronic address: amm2014@med.cornell.edu.
PMID: 35851487 DOI: 10.1016/j.blre.2022.100988
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.

Keywords

B cell; EZH2 inhibitor; Epigenomics; Lymphoma; Tazemetostat.

Figures
Products