Studies of Bioactivity, Conformation and Pharmacokinetic Profiles of Site-Specific PEGylated Thymosin Alpha 1 Derivatives

Site-specific mono-PEGylations were performed in different conformational regions of Thymosin alpha 1 (Tα1) by introducing one cysteine residue into the chosen site and coupling with thiol-specific mPEG-MAL reagent. Results demonstrated that PEGylated sites and regions influenced the conformations and pharmacokinetic profiles of the peptide greatly with following order: α-helix, β-turn, random coil and terminals, but little on the immunoactivity.