C-Terminally PEGylated hGH-derivatives
| Autor: | Anja K. Pedersen, Florencio Zaragoza, Trine R. Clausen, Kjeld Madsen, Magali Zundel, Sonja Bak, Niels Blume, Bernd Peschke |
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| Rok vydání: | 2007 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Polyethylene Glycols Catalysis chemistry.chemical_compound Capillary Electrochromatography Drug Discovery PEG ratio Humans Molecular Biology Chromatography High Pressure Liquid Human Growth Hormone C-terminus Organic Chemistry Biological activity Receptors Somatotropin Oxime Cycloaddition chemistry Spectrometry Mass Matrix-Assisted Laser Desorption-Ionization Click chemistry Molecular Medicine Indicators and Reagents Spectrophotometry Ultraviolet hormones hormone substitutes and hormone antagonists |
| Zdroj: | Bioorganic & Medicinal Chemistry. 15:4382-4395 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2007.04.037 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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