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Curr Oncol Rep. 2019 Feb 4;21(2):13. doi: 10.1007/s11912-019-0762-x.

BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer.

Author information

1
Medical Oncology, Oncology Institute of Southern Switzerland, Ospedale San Giovanni, 6500, Bellinzona, Switzerland.
2
Medical Oncology, Oncology Institute of Southern Switzerland, Ospedale San Giovanni, 6500, Bellinzona, Switzerland. anastasios.stathis@eoc.ch.

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. 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.

KEYWORDS:

Bromodomain and extraterminal motif proteins inhibitor (BETi); Enhancer of zeste homolog 2 inhibitor (EZH2i); Epigenetic agents; Hematological malignancies; Solid tumors

PMID:
30715616
DOI:
10.1007/s11912-019-0762-x

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