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Bromodomain and Extra-Terminal domain inhibitors for lymphoid malignancies

Bertoni, Francescoa; Stathis, Anastasiosb

Current Opinion in Hematology: July 2019 - Volume 26 - Issue 4 - p 273–280
doi: 10.1097/MOH.0000000000000519
LYMPHOID BIOLOGY AND DISEASES: Edited by Ari M. Melnick
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Purpose of review Pharmacological inhibition of Bromodomain and Extra-Terminal (BET) domain proteins is a very exciting epigenetic therapeutic modality. Due to the central role of BET proteins in transcription regulation, their inhibition heavily affects lymphoma cells and BET inhibitors show a clear preclinical antitumor activity as single agents and in combination, paired with early reports of clinical activity.

Recent findings Relevant data have been recently presented on the mechanism of action of the BET inhibitors, on modalities to improve their activity in lymphomas, and their clinical evaluation.

Summary There are now plenty of preclinical data sustaining BET proteins as therapeutic targets in lymphomas. Newer compounds and combinations with other agents may be pursued in the future aiming also to identify those patients that they most likely benefit from BET inhibition.

aUniversità della Svizzera italiana, Istituto Oncologico di Ricerca

bOncology Institute of Southern Switzerland, Bellinzona, Switzerland

Correspondence to Professor Francesco Bertoni, MD, Institute of Oncology Research, via Vincenzo Vela 6, 6500 Bellinzona, Switzerland. Tel: +41 91 8200 367; fax: +41 91 8200 397; e-mail: francesco.bertoni@ior.usi.ch

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