Choon Woo Lim

Antibody functionalization with a dual reactive hydrazide/click crosslinker.

A water-soluble, dual reactive hydrazide/click crosslinker (ethynyl hydrazide, EH) was synthesized and characterized. A model antibody, human immunoglobulin G (hIgG), was ethynylated by conventional oxidation/hydrazide reactions with the hydrazide moiety of EH. The terminal alkyne conjugated to the glycan of hIgG was easily functionalized by quantitative and bioorthogonal Cu(I)-catalyzed azide-alkyne cycloaddition. The potential of the hydrazide/click crosslinker as a reagent to functionalize antibodies was demonstrated with fluorophore labeling and antibody immobilization.

Small molecular weight PEGylation of diosgenin in an in vivo animal study for diabetic auditory impairment treatment

Diosgenin was modified to control its in vivo bioavailability by conjugating a hydrophilic unit, tetraethylene glycol. The diosgenin-tetraethylene glycol conjugate (TE) was orally administered in streptozotocin induced diabetic mice for this auditory protection study. The bioactivity improvement of TE for in vivo diabetic auditory impairment treatment was clearly observed in three different auditory tests and compared with that of diosgenin. The improvement in in vivo efficacy suggests that the small molecular weight PEGylation of diosgenin is a synthetically robust and systematically applicable strategy to reform the poor pharmacokinetics of a hydrophobic aglycone.