Site-specific PEGylation of a lysine-deficient TNF-α with full bioactivity

@article{Yamamoto2003SitespecificPO,
  title={Site-specific PEGylation of a lysine-deficient TNF-α with full bioactivity},
  author={Yoko Yamamoto and Yasuo M Tsutsumi and Yasuo Yoshioka and Toshihide Nishibata and Kyoko Kobayashi and Takayuki Okamoto and Yohei Mukai and Tomoe Shimizu and Shinsaku Nakagawa and Satoshi Nagata and Tadanori Mayumi},
  journal={Nature Biotechnology},
  year={2003},
  volume={21},
  pages={546-552}
}
Addition of polyethylene glycol to protein (PEGylation) to improve stability and other characteristics is mostly nonspecific and may occur at all lysine residues, some of which may be within or near an active site. Resultant PEGylated proteins are heterogeneous and can show markedly lower bioactivity. We attempted to develop a strategy for site-specific mono-PEGylation using tumor necrosis factor-α (TNF-α). We prepared phage libraries expressing TNF-α mutants in which all the lysine residues… CONTINUE READING
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