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Updated: Mar 14, 2026

Genetic Encoding of a Non-Canonical Amino Acid for the Generation of Antibody-Drug Conjugates Through a Fast Bioorthogonal Reaction
Published on: September 14, 2018
2-Deoxystreptamine Conjugates by Truncation-Derivatization of Neomycin
M Waqar Aslam1, Leandro C Tabares2, Alessio Andreoni2
1Radboud University Nijmegen, IMM Organic Chemistry, Heyendaalseweg 135, 6525 AJ, Nijmegen, the Netherlands.
Abstract:
A small library of truncated neomycin-conjugates is prepared by consecutive removal of 2,6-diaminoglucose rings, oxidation-reductive amination of ribose, oxidation-conjugation of aminopyridine/aminoquinoline and finally dimerization. The dimeric conjugates were evaluated for antibacterial activity with a unique hemocyanin-based biosensor. Based on the outcome of these results, a second-generation set of monomeric conjugates was prepared and found to display significant antibacterial activity, in particular with respect to kanamycin-resistant E. coli.
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