Inside HDACs with more selective HDAC inhibitors

被引:263
作者
Roche, Joelle [1 ,3 ]
Bertrand, Philippe [2 ,3 ]
机构
[1] Univ Poitiers, Equipe SEVE Sucres & Echanges Vegetaux Environm, Lab Ecol & Biol Interact, CNRS,UMR 7267, F-86073 Poitiers 09, France
[2] CNRS, UMR 7285, Inst Chim Milieux & Mat Poitiers, 4 Rue Michel Brunet,TSA 51106,B28, F-86073 Poitiers 09, France
[3] Reseau Epigenet Canc Pole Grand Ouest, Brest, France
关键词
Epigenetics; HDAC inhibitors; Synthesis; Molecular modelling; Histone acetylation; HISTONE DEACETYLASE INHIBITORS; SUBEROYLANILIDE HYDROXAMIC ACID; BIOLOGICAL EVALUATION; NITRIC-OXIDE; CLASS-I; STRUCTURAL REQUIREMENTS; ANTICANCER ACTIVITIES; ISOFORM-SELECTIVITY; LARGAZOLE ANALOGS; POTENTIAL THERAPY;
D O I
10.1016/j.ejmech.2016.05.047
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Inhibitors of histone deacetylases (HDACs) are nowadays part of the therapeutic arsenal mainly against cancers, with four compounds approved by the Food and Drug Administration. During the last five years, several groups have made continuous efforts to improve this class of compounds, designing more selective compounds or compounds with multiple capacities. After a survey of the HDAC biology and structures, this review summarizes the results of the chemists working in this field, and highlights when possible the behavior of the molecules inside their targets. (C) 2016 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:451 / 483
页数:33
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