Three-Dimensional Structural Diversity-Oriented Peptidomimetics Based on the Cyclopropylic Strain
Three-Dimensional Structural Diversity-Oriented Peptidomimetics Based on the Cyclopropylic Strain
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DOI：
10.1021/ol400469w
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发表时间：
2013-04-05
期刊：
影响因子：
5.2
通讯作者：
Shuto, Satoshi
中科院分区：
文献类型：
--
作者：
Mizuno, Akira;Miura, Shiho;Shuto, Satoshi
基于环丙烷的结构特征，即环丙基菌株，设计了包含具有三维结构多样性的8个立体异构体支架的构象限制性肽模拟物，其模拟了覆盖β-转角至β-链的广泛的四肽构象。立体选择性合成所设计的肽模拟物导致非肽黑皮质素-4受体配体的鉴定。
Conformationally restricted peptidomimetics comprising eight stereoisomeric scaffolds with three-dimensional structural diversity were designed based on the structural features of cyclopropane, that is, cyclopropylic strain, which mimic wide-ranging tetrapeptide conformations covering beta-turns through beta-strands. Stereoselective synthesis of the designed peptidomimetics led to the identification of nonpeptidic melanocortin-4 receptor ligands.