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General dual functionalisation of biomacromolecules via a cysteine bridging strategy

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Abstract

Site-selective modification of peptides and proteins has resulted in the development of a host of novel tools for the study of cellular systems or the synthesis of enhanced biotherapeutics. There is a need for useful methodologies that enable site-selective modification of native peptides or proteins, which is even more prevalent when modification of the biomolecule with multiple payloads is desired. Herein, we report the development of a novel dual functional divinylpyrimidine (dfDVP) platform that enables robust and modular modification of peptides, antibody fragments and antibodies. These biomacromolecules could be easily functionalised with a range of functional payloads (e.g. fluorescent dyes, cytotoxic warheads or cell-penetrating tags). Importantly, the dual functionalised peptides and antibodies demonstrated exquisite bioactivity in a range of in vitro cellular assays, showcasing the enhanced utility of these bioactive conjugates.

Graphical abstract: General dual functionalisation of biomacromolecules via a cysteine bridging strategy

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Supplementary files

Article information


Submitted
30 Apr 2020
Accepted
14 May 2020
First published
14 May 2020

This article is Open Access

Org. Biomol. Chem., 2020, Advance Article
Article type
Paper

General dual functionalisation of biomacromolecules via a cysteine bridging strategy

S. J. Walsh, J. Iegre, H. Seki, J. D. Bargh, H. F. Sore, J. S. Parker, J. S. Carroll and D. R. Spring, Org. Biomol. Chem., 2020, Advance Article , DOI: 10.1039/D0OB00907E

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