期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 18, 期 22, 页码 4224-4230出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0ob00907e
关键词
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资金
- AstraZeneca
- Cambridge Trusts
- EPSRC [EP/P020291/1]
- Trinity College Cambridge
- GlaxoSmithKline/EPSRC
- Royal Society (Wolfson Research Merit Award)
- EPSRC [EP/P020291/1] Funding Source: UKRI
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 ofin vitrocellular assays, showcasing the enhanced utility of these bioactive conjugates.
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