Drug Metabolism Letters

Author(s): Jiankun Qie, Jinbo Ma, Liangyou Wang, Xiaoyu Xu, Jianquan Zheng, Sijian Dong, Jianwei Xie, Huixian Sun, Wenxia Zhou, Chunhui Qi, Xiunan Zhao, Yongxiang Zhang and Keliang Liu

DOI: 10.2174/187231207781369780

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

Page: [232 - 340] Pages: 109

  • * (Excluding Mailing and Handling)

Abstract

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.

Keywords: Site-specific PEGylation, thymosin alpha 1, immunoactivity