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Modified antibiotic peptides having variable systemic release
专利权人:
Nicole Berthold;Friederike Nollmann;Ralf Hoffmann
发明人:
Ralf Hoffmann,Nicole Berthold,Friederike Nollmann
申请号:
US14128083
公开号:
US20140309161A1
申请日:
2012.06.20
申请国别(地区):
US
年份:
2014
代理人:
摘要:
The invention relates to modified antibiotic peptides, in particular derivatives of apidaecin and oncocin, preferably having increased stability, reduced immunoreaction, and improved pharmacokinetics. In the invention, the peptide antibiotics are reversibly protected by means of a linker having the polymer polyethylene glycol (PEG). The peptide linker contains a recognition sequence for trypsin-like serum proteases. In the apidaecin derivatives, the linker and the PEG are bonded to a side chain. In the serum, the linker is cut by serum proteases and PEG is separated off. The released peptide still contains remnants of the linker, which are still bonded to the amino group in the side chain. Astonishingly, said remaining remnants of the linker impair the activity of the antimicrobial peptide only a little or not at all.
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