Bicyclic peptides as potent inhibitors of histone deacetylases: Optimization of alkyl loop length

Bicyclic peptides as potent inhibitors of histone deacetylases: Optimization of alkyl loop length
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DOI:
10.1016/j.bmcl.2009.12.054
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发表时间:
2010-02-01
影响因子:
2.7
通讯作者:
Yoshida, Minoru
Yoshida, Minoru
中科院分区:
医学4区
文献类型:
--
作者:
Islam, Nurul M.;Kato, Tamaki;Yoshida, Minoru

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合成了双环四肽异羟肟酸作为组蛋白脱乙酰酶(HDAC)抑制剂,对其抑制活性的评价表明,它们对HDAC1和HDAC4具有较强的抑制活性。在体内的活性依赖于烷基环长。(C)2009爱思唯尔有限公司。保留所有权利。
Bicyclic tetrapeptide hydroxamic acids were prepared as histone deacetylase (HDAC) inhibitors, and the evaluated inhibitory activity shows that they are potent against HDAC1 and HDAC4. The in vivo activity depends on alkyl loop length. (c) 2009 Elsevier Ltd. All rights reserved.