Discovery of peptidic miR-21 processing inhibitor by mirror image phage display: A novel method to generate RNA binding D-peptides
Discovery of peptidic miR-21 processing inhibitor by mirror image phage display: A novel method to generate RNA binding D-peptides
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DOI：
10.1016/j.bmcl.2017.01.023
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发表时间：
2017-02-15
影响因子：
2.7
通讯作者：
Umemoto, Tadashi
中科院分区：
文献类型：
--
作者：
Sakamoto, Kotaro;Otake, Kentaro;Umemoto, Tadashi
发展了一种新的制备RNA结合D肽的方法。为了实现筛选方法，将噬菌体展示应用于“镜像”RNA（RNA的L-对映体）。我们选择pre-miR 21作为初始筛选靶标来证明该方法。成功获得镜像的pre-miR-21结合肽序列，并使用n-氨基酸化学合成。D-肽预期具有作为药物候选物的有利性质，例如蛋白酶抗性和低免疫原性。作为D-肽与pre-miR-21的结合评价的结果，EC 50值为440 nM。此外，该o肽对miR-21的加工具有抑制活性。(C)2017爱思唯尔有限公司版权所有
A novel method to generate RNA binding D-peptide has been developed. To achieve the screening method, phage display was applied to "Mirrored" RNA (L-enantiomer of RNA). We have selected pre-miR21 as an initial screening target to demonstrate the method. The mirrored pre-miR-21 binding peptide sequences were successfully obtained, and were chemically synthesized using n-amino acids. D-peptide is expected to have favorable properties as a drug candidate such as protease resistance and low immunogenicity. As a result of binding evaluation of the D-peptide to pre-miR-21, the EC50 value was 440 nM. In addition, the o-peptide possessed inhibition activity to miR-21 processing. (C) 2017 Elsevier Ltd. All rights reserved.