Page 50 - Tyrosine-Based Bioconjugations - Jorick Bruins
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Chapter 2
2.3. Conclusion
We have successfully developed a site-specific bioconjugation method based on the in situ enzymatic oxidation of tyrosine by mushroom tyrosinase. Various BCN derivatives were successfully conjugated to C-terminal, oxidized tyrosine residues via SPOCQ. This cycloaddition occurs quickly, selectively, and under physiological conditions on a variety of proteins. Extensive optimization of reaction conditions is anticipated to allow fully selective and quantitative conversion. Research along those lines is currently ongoing in our laboratories. We envision that SPOCQ on tyrosine residues can be a valuable tool to create more unique, orthogonal conjugation possibilities for a wide variety of protein modifications, including the preparation of next-generation, site-specifically generated antibody–drug conjugates.
2.4. Supporting information
This work can be found at https://pubs.acs.org/doi/10.1021/acs.bioconjchem.7b00046. Further permissions related to the material excerpted should be directed to the ACS
The Supporting Information is available free of charge.
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