Bis-sulfone-PEG4-m contains a bis-sulfone group and a polyethylene glycol (PEG) moiety. The bis-sulfone compound is a highly reactive bidentate alkylation reagent. It readily react with two cysteine thiols that is derived from reduction of the disulfide bridge on protein/antibody to form site specific conjugation. The mPEG24 is used to improve the solubility and stability of the compound in solution, allowing it to be more easily conjugated to biologics.
In bioconjugation, Bis-sulfone alkylating labeling involves two steps: 1. disulfide reduction to release the two cysteine thiols and 2. re-forming a three-carbon bridge by bis-alkylation to which other functional group is covalently attached. This process avoids the potential irreversible denaturation of the proteins by maintaining their tertiary structure. This bis-sulfone approach, together with the dibromo-maleimide approach, offers biologists a great tool for site specific bioconjugation that impairs no or least biological activities.
The PEG-bis-sulfone can also undergoes site-specific conjugation to the histidines in C or N-terminal tag without metal chelation. The site selective PEGylation between the poly-histidine tag (His-tag) bearing protein and PEG-bis-sulfone through a bis-alkylation process represents a promising conjugation approach that retains the biological activity after protein modification/purification.* (see Selected References section).
*https://pubs.rsc.org/en/content/articlehtml/2019/sc/c8sc03355b
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