Engineering Enzyme-Cleavable Oligonucleotides by Automated Solid-Phase Incorporation of Cathepsin B Sensitive Dipeptide Linkers,Angewandte Chemie International Edition

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Engineering Enzyme-Cleavable Oligonucleotides by Automated Solid-Phase Incorporation of Cathepsin B Sensitive Dipeptide Linkers
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2021-12-25 , DOI: 10.1002/anie.202114016
Cheng Jin ₁ , Afaf H Ei-Sagheer _{1,

2} , Siqi Li ₃ , Katherine A Vallis ₃ , Weihong Tan _{4,

5} , Tom Brown ₁

Affiliation

Cathepsin B-sensitive dipeptide phosphoramidites were developed for automated synthesis of enzyme-cleavable oligonucleotides. The enzymatic cleavage of Val-Ala-02 by cathepsin B is efficient in the context of single-stranded DNA, but is sterically hindered by double-stranded DNA and short hairpin loops. The design of Val-Ala-Chalcone allows the construction of oligonucleotide–drug conjugates which release their small-molecule payload after enzymatic cleavage.

中文翻译：

通过组织蛋白酶 B 敏感二肽接头的自动固相掺入工程酶可切割的寡核苷酸

组织蛋白酶 B 敏感二肽亚磷酰胺被开发用于酶可切割寡核苷酸的自动合成。组织蛋白酶 B 对 Val-Ala-02 的酶促裂解在单链 DNA 中是有效的，但会受到双链 DNA 和短发夹环的空间阻碍。Val-Ala-Chalcone 的设计允许构建寡核苷酸-药物缀合物，在酶裂解后释放其小分子有效负载。

更新日期：2021-12-25

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