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一种用于制备多模态修饰肽成像探针的化学策略。

A Chemical Strategy for the Preparation of Multimodified Peptide Imaging Probes.

机构信息

Istituto di Biostrutture e Bioimmagini, Consiglio Nazionale Delle Ricerche, Via Pietro Castellino 111, 80131 Napoli, Italy.

Centro di Imaging Molecolare, Dipartimento di Biotecnologie Molecolari e Scienze per La Salute, Università di Torino, via Nizza 52, 10126 Torino, Italy.

出版信息

J Org Chem. 2023 Apr 7;88(7):4546-4553. doi: 10.1021/acs.joc.3c00014. Epub 2023 Mar 29.

Abstract

Multimodality probes appear of great interest for innovative imaging applications in disease diagnosis. Herein, we present a chemical strategy enabling site-specific double-modification and cyclization of a peptide probe exploiting native chemical ligation (NCL) and thiol-maleimide addition. The synthetic strategy is straightforward and of general applicability for the development of double-labeled peptide multimodality probes.

摘要

多模态探针在疾病诊断的创新成像应用中似乎具有很大的兴趣。在此,我们提出了一种化学策略,利用天然化学连接(NCL)和硫醇-马来酰亚胺加成,实现肽探针的定点双修饰和环化。该合成策略简单直接,适用于双标记肽多模态探针的开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2746/10088022/2c522f16921d/jo3c00014_0001.jpg

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