4.7 Review

Dysregulation of histone methyltransferases in breast cancer - Opportunities for new targeted therapies?

Journal

MOLECULAR ONCOLOGY
Volume 10, Issue 10, Pages 1497-1515

Publisher

WILEY
DOI: 10.1016/j.molonc.2016.09.003

Keywords

Histone methyltransferase; Breast cancer; Chromatin; Transcription; Inhibitors

Categories

Funding

  1. Australian National Health and Medical Research Council (NHMRC) [1016701, 1024852, 1086727]
  2. NHMRC IRIISS
  3. Victorian State Government through VCA funding of the Victorian Breast Cancer Research Consortium
  4. Australian Cancer Research Foundation
  5. National Breast Cancer Foundation Career Development Fellowship
  6. NHMRC Australia Fellowship
  7. National Health and Medical Research Council of Australia [1086727] Funding Source: NHMRC
  8. National Breast Cancer Foundation [ECF-15-002] Funding Source: researchfish

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Histone methyltransferases (HMTs) catalyze the methylation of lysine and arginine residues on histone tails and non-histone targets. These important post-translational modifications are exquisitely regulated and affect chromatin compaction and transcriptional programs leading to diverse biological outcomes. There is accumulating evidence that genetic alterations of several HMTs impinge on oncogenic or tumor-suppressor functions and influence both cancer initiation and progression. HMTs therefore represent an opportunity for therapeutic targeting in those patients with tumors in which HMTs are dysregulated, to reverse the histone marks and transcriptional programs associated with aggressive tumor behavior. In this review, we describe the known histone methyltransferases and their emerging roles in breast cancer tumorigenesis. (C) 2016 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.

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