Bicyclic tetrapeptides as potent HDAC inhibitors: Effect of aliphatic loop position and hydrophobicity on inhibitory activity
Bicyclic tetrapeptides as potent HDAC inhibitors: Effect of aliphatic loop position and hydrophobicity on inhibitory activity
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DOI：
10.1016/j.bmc.2014.06.031
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发表时间：
2014-08-01
影响因子：
3.5
通讯作者：
Yoshida, Minoru
中科院分区：
文献类型：
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作者：
Islam, Md. Nurul;Islam, Md. Shahidul;Yoshida, Minoru
Several histone deacetylase (HDAC) inhibiting bicyclic tetrapeptides have been designed and synthesized through intramolecular ring-closing metathesis (RCM) reaction and peptide cyclization. We designed bicyclic tetrapeptides based on CHAP31, trapoxin B and HC-toxin I. The HDAC inhibitory and p21 promoter assay results showed that the aliphatic loop position as well as the hydrophobicity plays an important role toward the activity of the bicyclic tetrapeptide HDAC inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.
