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Updated: May 23, 2026

Genetic Encoding of a Non-Canonical Amino Acid for the Generation of Antibody-Drug Conjugates Through a Fast Bioorthogonal Reaction
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タイロシンにおけるペプチドの直接的生物結合/PEGylationは,線形および分岐型ポリマー型ダイアゾニウム塩によるものです

Mathew W Jones1, Giuseppe Mantovani, Claudia A Blindauer

  • 1Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK.

Journal of the American Chemical Society
|April 13, 2012
PubMed
まとめ

この研究では,ペプチドチロシン残留物に対するサイト固有のポリマー結合が示され,薬物の投与を向上させています. その結果生成されたコンジュガートは,in vitroおよびin vivoで生物学的活性を維持した.

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A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
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The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para position.