Drug Metabolism Letters

Zhiyang Zhao
Amgen
Cambridge, MA
USA

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

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, Keliang Liu.

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

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Article Details

VOLUME: 1
ISSUE: 3
Year: 2007
Page: [232 - 340]
Pages: 109
DOI: 10.2174/187231207781369780
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