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BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer

  • Evolving Therapies (RM Bukowski, Section Editor)
  • Published:
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Abstract

Purpose of Review

Increasing evidence suggests that epigenome plays a central role in cancer development making it a promising target for anticancer treatments. Here, we review two new classes of epigenome-targeting agents: the bromodomain and extraterminal domain proteins (BET) inhibitors and the enhancer of zeste homolog (EZH2) inhibitors.

Recent Findings

Clinical research evaluating BET and EZH2 inhibitors is still at an early stage; however, both classes of drugs have demonstrated activity among different hematologic malignancies and solid tumors.

Summary

Several studies on BETi and EZH2i are ongoing to better define their potential role in cancer treatment, which patients are most likely to benefit and if the association with other drugs can improve their efficacy.

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  1. Sofia Genta and Maria Cristina Pirosa contributed equally to this work.

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  1. Medical Oncology, Oncology Institute of Southern Switzerland, Ospedale San Giovanni, 6500, Bellinzona, Switzerland

    Sofia Genta, Maria Cristina Pirosa & Anastasios Stathis

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  1. Sofia Genta
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Sofia Genta declares that she has no conflict of interest.

Maria Cristina Pirosa declares that she has no conflict of interest.

Anastasios Stathis has received research funding (paid to his institution) from Amgen, Bayer, Novartis, Pfizer, Roche, and MEI Pharma, and has received travel grants from AbbVie and PharmaMar.

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Genta, S., Pirosa, M.C. & Stathis, A. BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer. Curr Oncol Rep 21, 13 (2019). https://doi.org/10.1007/s11912-019-0762-x

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