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Submonomer Solid-Phase Aza-peptide Synthesis and Circular Dichroism Spectroscopic Analysis of aza-Phe~4-GHRP-6

机译:柳叶固相α-肽合成及圆形二色性光谱分析AZA-PHE〜4 -GHRP-6

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摘要

Aza-peptides incorporate an aza-amino acid residue (in which N replaces the alpha-CH) into the peptide backbone. They have improved peptide pharmacokinetic properties and enhanced substrate activity and specificity towards receptor targets [1], likely because of lone pair interactions of the hydrazine nitrogen causing a pre-organized backbone secondary structure related to P-turn types [2]. Aza-peptides are useful probes for exploring the influences of peptide backbone configuration and conformation on the biological activity of the native peptide.
机译:AZA-肽掺入AZA-氨基酸残基(其中N替换α-CH)进入肽骨架中。它们具有改善的肽药代动力学性能和增强的基底活性和对受体靶标的特异性[1],可能因为肼氮的孤立相互作用导致与p匝类型相关的预组织的骨干二级结构[2]。 AZA肽是探索肽骨架配置和构象对天然肽生物活性的有用探针。

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