Studies of bioactivity, conformation and pharmacokinetic profiles of site-specific PEGylated thymosin alpha 1 derivatives.

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

Index: Drug Metab. Lett. 1 , 232-240, (2007)

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Abstract

Site-specific mono-PEGylations were performed in different conformational regions of Thymosin alpha 1 (T alpha 1) 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: alpha-helix, beta-turn, random coil and terminals, but little on the immunoactivity.