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Peptide-Assisted Design of Peptoid Sequences: One Small Step in Structure and Distinct Leaps in Functions
ACS Macro Letters ( IF 5.8 ) Pub Date : 2020-01-31 , DOI: 10.1021/acsmacrolett.9b00977
Eva Maron 1 , Zdravko Kochovski 2 , Ronald N Zuckermann 3 , Hans G Börner 1
Affiliation  

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 meta-tetra(hydroxyphenyl)-chlorin. A set of peptoid-block-poly(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.

中文翻译:

肽类序列的肽辅助设计:结构上的一小步和功能上的明显飞跃

使用肽序列设计功能性 peptoids 已被证明是一种基于肽的配方添加剂,该添加剂专门用于溶解光敏剂-四(羟苯基)-二氢卟酚。一组 peptoid -block-合成具有系统序列变化的聚(乙二醇)增溶剂,以揭示侧链序列和骨架功能对药物宿主和释放特性的贡献。药物有效载荷敏感地依赖于侧链模式,性能最佳的类肽序列的容量是相应肽的 3 倍。与肽类似物相比,拟肽骨架不仅充当中性支架,而且通过降低协助药物转移到血浆蛋白模型的能力来影响药物释放动力学。
更新日期:2020-02-03
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