Figure: Schematic diagram of the conjugation reaction for Cov-X-body (PNAS, 2010)
The Cov-X-body prototype was firstly developed based on an integrin targeting pharmacophore. Generally, a Cov-X-body is composed of a scaffold antibody and pharmacophore peptide heterodimers. People can use the approach of “chemical programming” to covalently modify antibodies so as to generate and optimize bispecific antibodies rapidly. In this versatile strategy, two small molecules are joined into a heterodimer by a branched linker and subsequently site-specifically conjugated to the scaffold antibody. In a Cov-X-antibody molecule, the pharmacophores have functional activities while the scaffold antibody contributes to the long serum half-life and Ig-like distribution.
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