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公开(公告)号：US09387255B2
公开(公告)日：2016-07-12
申请号：US14128083
申请日：2012-06-20
IPC分类号： A61K38/16 , A61K38/10 , C07K14/435 , C07K7/08 , A61K47/48 , A01N37/46 , A01N63/02 , C12Q1/37 , A01N25/22 , A61K38/00
CPC分类号： C07K14/43572 , A01N25/22 , A01N37/46 , A01N63/02 , A61K38/00 , A61K38/10 , A61K38/16 , A61K38/1767 , A61K47/60 , C07K7/08 , C07K11/00 , C07K14/43563 , C12Q1/37
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.
摘要翻译： 本发明涉及修饰的抗生素肽，特别是apidaecin和oncocin的衍生物，优选具有增加的稳定性，降低的免疫反应和改善的药代动力学。 在本发明中，肽抗生素通过具有聚合物聚乙二醇（PEG）的接头可逆地保护。 肽接头包含胰蛋白酶样血清蛋白酶的识别序列。 在apidaecin衍生物中，接头和PEG与侧链结合。 在血清中，用血清蛋白酶切割接头，分离出PEG。 释放的肽仍然含有仍然与侧链中的氨基键合的接头残基。 令人惊讶的是，所述接头的剩余残留物仅仅少量地损害了抗微生物肽的活性。
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公开(公告)号：US20140309161A1
公开(公告)日：2014-10-16
申请号：US14128083
申请日：2012-06-20
CPC分类号： C07K14/43572 , A01N25/22 , A01N37/46 , A01N63/02 , A61K38/00 , A61K38/10 , A61K38/16 , A61K38/1767 , A61K47/60 , C07K7/08 , C07K11/00 , C07K14/43563 , C12Q1/37
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.
摘要翻译： 本发明涉及修饰的抗生素肽，特别是apidaecin和oncocin的衍生物，优选具有增加的稳定性，降低的免疫反应和改善的药代动力学。 在本发明中，肽抗生素通过具有聚合物聚乙二醇（PEG）的接头可逆地保护。 肽接头包含胰蛋白酶样血清蛋白酶的识别序列。 在apidaecin衍生物中，接头和PEG与侧链结合。 在血清中，用血清蛋白酶切割接头，分离出PEG。 释放的肽仍然含有仍然与侧链中的氨基键合的接头残基。 令人惊讶的是，所述接头的剩余残留物仅仅少量地损害了抗微生物肽的活性。
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