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Site-Selective Synthesis of Insulin Azides and Bioconjugates

Author:
Boga, Sobhana Babu  Krska, Shane W.  Lin, Songnian  Pissarnitski, Dmitri  Yan, Lin  Kekec, Ahmet  Tang, Weijuan  Pierson, Nicholas A.  Strulson, Christopher A.  Streckfuss, Eric  Zhu, Xiaohong  Zhang, Xiaoping  Kelly, Terri  Parish, Craig A.  


Journal:
BIOCONJUGATE CHEMISTRY


Issue Date:
2019


Abstract(summary):

A synthetic method to access novel azido-insulin analogs directly from recombinant human insulin (RHI) was developed via diazo-transfer chemistry using imidazole-1-sulfonyl azide. Systematic optimization of reaction conditions led to site-selective azidation of amino acids B1-phenylalanine and B29-lysine present in RHI. Subsequently, the azido-insulin analogs were used in azide-alkyne [3 + 2] cycloaddition reactions to synthesize a diverse array of triazole-based RHI bioconjugates that were found to be potent human insulin receptor binders. The utility of this method was further demonstrated by the concise and controlled synthesis of a heterotrisubstituted insulin conjugate.


Page:
1127---1132


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