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C-Terminally PEGylated hGH-derivatives
Bernd Peschke1, Magali Zundel, Sonja Bak
1Protein Engineering, Novo Nordisk A/S, Novo Nordisk Park, 2760 Maaloev, Denmark. bpes@novonordisk.com
Abstract:
A two-step strategy was used for the preparation of C-terminally PEGylated hGH-derivatives. In a first step a CPY-catalyzed transpeptidation was performed on hGH-Leu-Ala, introducing reaction handles, which were used in the second step for the ligation of PEG-moieties. Both oxime-ligation and copper(I) catalyzed [2+3]-cycloaddition reactions were used for the attachment of PEG-moieties. The biological data show a dependency of the potency of the hGH-derivatives on both size as well as shape of the PEG-group.
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