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The excellent molecular recognition capabilities of monoclonal antibodies (mAbs) have opened up exciting opportunities for biotherapeutic discovery. Taking advantage of the full potential of this tool necessitates affinity ligands capable of conjugating directly with small molecules to a defined degree of biorthogonality, especially when modifying natural Abs. Herein, a bioorthogonal boronate‐affinity‐based...
A boronic acid based biorthogonal probe in combination with an acyl donor has been introduced that enables site‐specific incorporation of azide group at the Ser and Tyr residues of nonengineered full‐length antibody. Further derivatization of this functional site was accomplished through click reaction, yielding well‐defined immunoconjugates. The generality of this boronate‐affinity method has been...
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