Maron Eva, Kochovski Zdravko, Zuckermann Ronald N, Börner Hans G
Department of Chemistry, Laboratory for Organic Synthesis of Functional Systems, Humboldt-Universität zu Berlin, Brook-Taylor-Str. 2, 12489 Berlin, Germany.
Soft Matter and Functional Materials, Helmholtz-Zentrum Berlin für Materialien und Energie, Hahn-Meitner-Platz 1, 14109 Berlin, Germany.
ACS Macro Lett. 2020 Feb 18;9(2):233-237. doi: 10.1021/acsmacrolett.9b00977. Epub 2020 Jan 31.
Using peptide sequences for the design of functional peptoids is demonstrated for a peptide-based formulation additive that was specifically tailored to solubilize the photosensitizer -tetra(hydroxyphenyl)-chlorin. A set of peptoidpoly(ethylene glycol) solubilizers with systematic sequence variations are synthesized to reveal contributions of side-chain sequence and backbone functionalities on drug hosting and release properties. The drug payload sensitively depends on the side-chain patterns, and the best performing peptoid sequence reaches 3-times higher capacity than the corresponding peptide. The peptoid backbone not only acts as a neutral scaffold but also impacts the drug release kinetics compared to the analogues peptide, by reducing the capability to assist drug transfer to blood plasma protein models.
利用肽序列设计功能性类肽，已在一种基于肽的制剂添加剂中得到验证，该添加剂是专门为增溶光敏剂四（羟基苯基）二氢卟酚而设计的。合成了一组具有系统序列变化的类肽 - 聚乙二醇增溶剂，以揭示侧链序列和主链功能对药物包载和释放特性的影响。药物负载量敏感地取决于侧链模式，性能最佳的类肽序列的载药能力比相应的肽高出3倍。与类似肽相比，类肽主链不仅作为中性支架，还通过降低协助药物转移至血浆蛋白模型的能力来影响药物释放动力学。
