Design and synthesis of AApeptides: A new class of peptide mimics
Design and synthesis of AApeptides: A new class of peptide mimics
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DOI：
10.1016/j.bmcl.2011.01.005
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发表时间：
2011-03-01
影响因子：
2.7
通讯作者：
Cai, Jianfeng
中科院分区：
文献类型：
--
作者：
Hu, Yaogang;Li, Xiaolong;Cai, Jianfeng
提出了一种新的肽类模拟物，称为“AApeptides”，它是n -酰化- n -氨基乙基氨基酸的低聚物。介绍了AApeptides的设计和高效合成。作为概念验证，我们发现AApeptides可以抑制p53/MDM2蛋白-蛋白相互作用，并且具有显著的活性（IC50 = 38 μ M）和特异性。初步数据还表明AApeptides抵抗酶水解。由于易于合成和多样化，具有强大的生物活性和抗蛋白质水解能力，序列特异性的AApeptides的开发可能会扩大其潜在的生物医学应用。(C) 2011 Elsevier Ltd.版权所有。
A new family of peptide mimics termed 'AApeptides', which are oligomers of N-acylated-N-aminoethyl amino acids, was proposed. The design and efficient synthesis of AApeptides are described. As proof-of-the-concept, we show that AApeptides can inhibit p53/MDM2 protein-protein interaction with significant activity (IC50 = 38 mu M) and specificity. Preliminary data also demonstrates that AApeptides are resistant to enzymatic hydrolysis. With the ease of synthesis and diversification, potent bioactivity, and resistance to proteolysis, the development of sequence-specific AApeptides may expand the potential biomedical applications of peptidomimetics. (C) 2011 Elsevier Ltd. All rights reserved.