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一种 rink 酰胺可溶性载体:高纯度 conotoxin 和其他肽,只需最少的试剂即可获得。

A rink-amide soluble support: high purity conotoxins and other peptides accessed with minimal reagents.

机构信息

Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai, Maharashtra 400076, India.

Department of Chemistry, Indian Institute of Technology Madras, Chennai, Tamil Nadu 600036, India.

出版信息

Org Biomol Chem. 2019 Aug 14;17(30):7238-7246. doi: 10.1039/c9ob01214a. Epub 2019 Jul 22.

Abstract

The use of peptides as therapeutics has been growing due to their biocompatibility. Solid phase peptide synthesis typically used to access these peptides requires excess reagents and/or microwave irradiation to drive reactions to completion because the reaction medium is heterogeneous. Reported herein is a soluble polynorbornene support containing rink amide attached sites for synthesizing oligopeptides and conotoxins in high purity using only 1.2 to 2 equivalents of coupling reagents. The support can be isolated as a precipitate from the reaction medium by adding ether. The loading capacity of the support can be easily determined by spectroscopy and can also be tuned by varying the monomer ratio. This support is promising for accessing peptides as the methodology uses minimal reagents and by-products can be easily separated.

摘要

由于其生物相容性,肽类作为治疗药物的应用越来越广泛。通常用于获得这些肽的固相肽合成需要过量的试剂和/或微波辐射来驱动反应完成,因为反应介质是不均匀的。本文报道了一种可溶性聚降冰片烯载体,其中含有 rink 酰胺连接位点,可仅使用 1.2 至 2 当量的偶联试剂,以高纯度合成寡肽和 conotoxin。通过添加乙醚,可将载体从反应介质中沉淀出来进行分离。通过光谱法可以很容易地确定载体的负载能力,并且通过改变单体的比例也可以对其进行调整。由于该方法使用的试剂最少,副产物很容易分离,因此这种载体在获得肽方面很有前景。

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