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一种使用酸不稳定连接子在固相中制备肽杂二聚体的策略。

A Strategy To Prepare Peptide Heterodimers in the Solid Phase with an Acid-Labile Linker.

机构信息

Beijing institute of Radiation Medicine , Beijing 100850 , P.R. China.

College of Engineering , Peking University , Beijing 100871 , P.R. China.

出版信息

Org Lett. 2019 Sep 20;21(18):7351-7355. doi: 10.1021/acs.orglett.9b02638. Epub 2019 Sep 3.

Abstract

The currently synthetic methods of peptide heterodimer involve tedious synthesis and purification steps. An acid-labile traceless linker was prepared, which is highly compatible with the Fmoc strategy and could be used to prepare peptide heterodimer on resin. The linker could be cleaved concomitantly with peptide cleavage, and two model heterodimers were synthesized. The proposed synthesis procedure is simple, straightforward, and provides great convenience for preparing disulfide-linked peptide heterodimers.

摘要

目前的肽杂二聚体的合成方法涉及繁琐的合成和纯化步骤。我们制备了一种酸不稳定的无痕连接子,它与 Fmoc 策略高度兼容,可以在树脂上用于制备肽杂二聚体。该连接子可以与肽切割同时进行切割,并且合成了两个模型杂二聚体。所提出的合成程序简单、直接,为制备二硫键连接的肽杂二聚体提供了极大的便利。

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