Faculty of Pharmaceutical Sciences, Center for Research and Education on Drug Discovery, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
Org Lett. 2013 Apr 5;15(7):1686-9. doi: 10.1021/ol400469w. Epub 2013 Mar 25.
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 β-turns through β-strands. Stereoselective synthesis of the designed peptidomimetics led to the identification of nonpeptidic melanocortin-4 receptor ligands.
设计了包含八个立体异构骨架的构象受限的肽类似物，这些骨架具有三维结构多样性，基于环丙烷的结构特征，即环丙基应变，模拟了广泛的四肽构象，涵盖了从β-转角到β-链的结构。设计的肽类似物的立体选择性合成导致了非肽类黑皮质素 4 受体配体的鉴定。
