University of Cologne, Department of Chemistry, Biochemistry, Zülpicher Str. 47a, D-50674 Cologne, Germany.
University of Cologne, Department of Chemistry, Organic Chemistry, Greinstraße 4, D-50939, Cologne, Germany.
Chem Commun (Camb). 2020 May 27;56(42):5685-5688. doi: 10.1039/d0cc01490g.
A series of linear and cyclic peptidomimetics composed of a cell-penetrating peptide and a non-natural, bifunctional 2,5-diketopiperazine scaffold is reported. Conformational studies revealed well-defined helical structures in micellar medium for linear structures, while cyclic peptidomimetics were more flexible. Biological investigations showed higher membrane-activity of cyclic derivatives allowing their use as shuttles for anti-cancer drugs.
报告了一系列由穿膜肽和非天然双功能 2,5-二酮哌嗪支架组成的线性和环状肽类似物。构象研究表明，线性结构在胶束介质中具有明确的螺旋结构，而环状肽类似物则更具柔性。生物学研究表明，环状衍生物具有更高的膜活性，可将其用作抗癌药物的载体。
