原创力文档overview of histone deacetylase inhibitors in haematological malignancies组蛋白脱乙酰酶抑制剂在血液学的恶性肿瘤的概述.pdfVIP
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overview of histone deacetylase inhibitors in haematological malignancies组蛋白脱乙酰酶抑制剂在血液学的恶性肿瘤的概述
Pharmaceuticals 2010, 3, 2674-2688; doi:10.3390/ph3082674
OPEN ACCESS
pharmaceuticals
ISSN 1424-8247
/journal/pharmaceuticals
Review
Overview of Histone Deacetylase Inhibitors in
Haematological Malignancies
Mark J. Bishton 1,*, Ricky W. Johnstone 1,3, Michael Dickinson 2, Simon Harrison 2 and
H. Miles Prince 2,3
1 Cancer Immunology Research, Peter MacCallum Cancer Centre, Melbourne, Australia
2 Department of Haematology and Medical Oncology, Peter MacCallum Cancer Centre, Australia
3 University of Melbourne, Parkville, Melbourne, Australia
* Author to whom correspondence should be addressed; E-Mail: Mark.Bishton@.
Received: 23 July 2010; in revised form: 12 August 2010 / Accepted: 13 August 2010/
Published: 17 August 2010
Abstract: Histone deacetylase inhibitors (HDACi) can induce hyperacetylation of both
histone and non-histone target resulting in epigenetic reprogramming and altered activity,
stability and localisation of non-histone proteins to ultimately mediate diverse biological
effects on cancer cells and their microenvironment. Clinical trials have demonstrated single
agent HDACi to have activity in hematological malignancies, in particular T-cell
lymphoma and Hodgkin lymphoma. Combination strategies with standard therapies based
on pre-clinical data are being employed with significant success due to their excellent side
effect profile. Correlative studies will provide valuable information on the sub-groups of
patients more likely to respond or be resistant to HDACi therapy, while long
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