Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

被引：1230

作者：

Falkenberg, Katrina J. ^{[1
]}

Johnstone, Ricky W. ^{[1
,2
]}

机构：

[1] Peter MacCallum Canc Ctr, Canc Therapeut Program, East Melbourne, Vic 3002, Australia

[2] Univ Melbourne, Sir Peter MacCallum Dept Oncol, Parkville, Vic 3052, Australia

来源：

NATURE REVIEWS DRUG DISCOVERY | 2014年 / 13卷 / 09期

基金：

澳大利亚国家健康与医学研究理事会;

关键词：

SUBEROYLANILIDE HYDROXAMIC ACID; TRANS-RETINOIC ACID; CELLS IN-VITRO; SPINAL MUSCULAR-ATROPHY; DOUBLE-STRAND BREAKS; VERSUS-HOST-DISEASE; HDAC INHIBITORS; GENE-EXPRESSION; VALPROIC ACID; EPIGENETIC REGULATION;

D O I：

10.1038/nrd4360

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Epigenetic aberrations, which are recognized as key drivers of several human diseases, are often caused by genetic defects that result in functional deregulation of epigenetic proteins, their altered expression and/or their atypical recruitment to certain gene promoters. Importantly, epigenetic changes are reversible, and epigenetic enzymes and regulatory proteins can be targeted using small molecules. This Review discusses the role of altered expression and/or function of one class of epigenetic regulators histone deacetylases (HDACs) - and their role in cancer, neurological diseases and immune disorders. We highlight the development of small-molecule HDAC inhibitors and their use in the laboratory, in preclinical models and in the clinic.

引用

页码：673 / 691

页数：19

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