Homogeneous Oligomeric Ligands Prepared via Radical Polymerization that Recognize and Neutralize a Target Peptide

Abiotic ligands that bind to specific biomolecules have attracted attention as substitutes for biomolecular ligands, such as antibodies and aptamers. Radical polymerization enables the production of robust polymeric ligands from inexpensive functional monomers. However, little has been reported abou...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2020-01, Vol.59 (2), p.679-683
Main Authors: Hoshino, Yu, Taniguchi, Shohei, Takimoto, Hinata, Akashi, Sotaro, Katakami, Sho, Yonamine, Yusuke, Miura, Yoshiko
Format: Article
Language:English
Subjects:
Antibodies
Aptamers
Biomolecules
block copolymers
combinatorial chemistry
Epitopes
Functional groups
homogeneous oligomer
Humans
Ligands
Monomers
Oligomers
Peptides
Peptides - chemistry
Polymerization
synthetic ligand
Target recognition
Toxicity
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Summary:Abiotic ligands that bind to specific biomolecules have attracted attention as substitutes for biomolecular ligands, such as antibodies and aptamers. Radical polymerization enables the production of robust polymeric ligands from inexpensive functional monomers. However, little has been reported about the production of monodispersed polymeric ligands. Herein, we present homogeneous ligands prepared via radical polymerization that recognize epitope sequences on a target peptide and neutralize the toxicity of the peptide. Taking advantage of controlled radical polymerization and separation, a library of multifunctional oligomers with discrete numbers of functional groups was prepared. Affinity screening revealed that the sequence specificity of the oligomer ligands strongly depended on the number of functional groups. The process reported here will become a general step for the development of abiotic ligands that recognize specific peptide sequences. Homogeneous oligomeric ligands that recognize epitope sequences on a target peptide and neutralize its toxicity have been prepared via radical polymerization of commercial bulk materials. These synthetic ligands, prepared by controlled radical polymerization, oligomer separation, and affinity screening, are an attractive alternative to biomolecular ligands.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201910558