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BET Bromodomain Inhibition as a Therapeutic Approach in Hematological Malignancies

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Histone Recognition

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Abstract

Pharmacological inhibition of BET proteins has emerged as an efficacious therapeutic strategy in a number of animal models of disease, including cancer, inflammation, fibrosis, and heart failure. The intense investigation of BET proteins as drug targets in recent years can be directly attributed to the widespread availability of potent and selective chemical probes with suitable pharmacokinetics for in vivo application. At the present time (late 2013), Phase I clinical trials have opened that will evaluate BET inhibitors developed by several independent groups. Several of these trials will be carried out in patients with hematopoietic cancers. Here, I will review the preclinical studies that have linked BET proteins to the pathogenesis of hematopoietic malignancy and the confluence of evidence suggesting that suppression of MYC expression underlies, at least in part, these therapeutic effects.

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  1. Cold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, NY, 11724, USA

    Christopher R. Vakoc

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  1. Christopher R. Vakoc
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Correspondence to Christopher R. Vakoc .

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  1. Department of Structural & Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, New York, USA

    Ming-Ming Zhou

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Vakoc, C.R. (2015). BET Bromodomain Inhibition as a Therapeutic Approach in Hematological Malignancies. In: Zhou, MM. (eds) Histone Recognition. Springer, Cham. https://doi.org/10.1007/978-3-319-18102-8_9

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