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一种具有特异性HER2受体结合能力的A9肽二聚体的无溶剂制备方法：增强结合亲和力的荧光光谱评估

Solvent-Free procedure of an A9 Peptide Dimer Exhibiting Specific HER2 Receptor Binding: Fluorescence Spectroscopy Evaluation of the Enhanced Binding Affinity.

作者信息

Verdoliva Valentina, Digilio Giuseppe, Iaccarino Emanuela, Luca Stefania De

机构信息

Institute of Crystallography, National Research Council (CNR), Via Vivaldi, 43, Caserta 81100, Italy.

Department of Science and Technological Innovation, Università del Piemonte Orientale "A. Avogadro", Alessandria 15121, Italy.

出版信息

J Med Chem. 2025 Aug 14;68(15):16299-16305. doi: 10.1021/acs.jmedchem.5c01194. Epub 2025 Jul 24.

DOI:10.1021/acs.jmedchem.5c01194
PMID:40704384
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12406181/
Abstract

HER2-expressing cancers currently benefit from targeted therapies, including monoclonal antibodies and antibody-drug conjugates that specifically bind to the extracellular domain of the receptor. Peptides targeting HER2 represent promising candidates for the development of alternative molecular drugs. In this study, we report a dimeric version of the previously validated A9 peptide as a ligand specifically targeting HER2. The novel A9-PEG-A9 conjugate consists of two A9 peptides whose N-terminal amino groups are linked via a polyethylene glycol chain. It was synthesized using a solvent-free protocol and validated as an improved ligand, demonstrating enhanced water solubility and increased affinity for the model receptor HER2-DIVMP, as determined by the fluorescence spectroscopy titration method.

摘要

目前，HER2表达型癌症可从靶向治疗中获益，这些治疗包括特异性结合该受体细胞外结构域的单克隆抗体和抗体-药物偶联物。靶向HER2的肽是开发替代分子药物的有前景的候选物。在本研究中，我们报告了先前已验证的A9肽的二聚体形式作为特异性靶向HER2的配体。新型A9-PEG-A9偶联物由两个A9肽组成，其N端氨基通过聚乙二醇链连接。它采用无溶剂方案合成，并被验证为一种改良配体，通过荧光光谱滴定法测定，其表现出增强的水溶性和对模型受体HER2-DIVMP的亲和力增加。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/f3dcf400895e/jm5c01194_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/fbc41192e3bc/jm5c01194_0008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/478cfb2f031b/jm5c01194_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/5b34246cab29/jm5c01194_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/f3dcf400895e/jm5c01194_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/fbc41192e3bc/jm5c01194_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/a298dfd2ea2d/jm5c01194_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/5e38d925e014/jm5c01194_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/a5d3edecbe86/jm5c01194_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/40856a382cbc/jm5c01194_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/478cfb2f031b/jm5c01194_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/5b34246cab29/jm5c01194_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e14/12406181/f3dcf400895e/jm5c01194_0007.jpg

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本文引用的文献

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