基本信息:
- 专利标题： ANTIMICROBIAL ALPHA-HELICAL CATIONIC POLYPEPTIDES
- 专利标题（中）：抗微生物ALPHA-HELICAL阳离子聚合物
- 申请号：PCT/US2016/039657 申请日：2016-06-27
- 公开(公告)号：WO2016210442A1 公开(公告)日：2016-12-29
- 发明人： CHENG, Jianjun , XIONG, Menghua , SONG, Ziyuan
- 申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
- 申请人地址： 352 Henry Administration Building 506 S. Wright Street Urbana, Illinois 61801 US
- 专利权人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
- 当前专利权人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
- 当前专利权人地址： 352 Henry Administration Building 506 S. Wright Street Urbana, Illinois 61801 US
- 代理机构： HAUKAAS, Michael H.
- 优先权： US62/185,345 20150626
- 主分类号： A61K38/00
- IPC分类号： A61K38/00 ; C07K2/00
摘要：
The invention provides antimicrobial polypeptides (AMPs) with high radial amphiphilicity. Unlike typical AMPs characterized by facial amphiphilicity or biomimetic antimicrobial polymers with randomly distributed charged and hydrophobic groups, these new AMPs are homo-polypeptides with radially amphiphilic structure. They adopt a stable ?-helical conformation with a hydrophobic helical core and a charged exterior shell, formed by flexible hydrophobic side chains with terminal charge group. The radially amphiphilic polypeptides offer several advantages over conventional AMPs with regard to stability against protease and simplicity of design. They also exhibit high antibacterial activity against both Gram-negative and Gram-positive bacteria and low hemolytic activity. The AMPs thus provide a general platform for treating drug-resistant bacterial infections.
摘要（中）：
本发明提供具有高径向两亲性的抗微生物多肽（AMP）。 不同于以面部两亲性为特征的典型AMP，具有随机分布的带电荷和疏水基团的仿生抗微生物聚合物，这些新的AMP是具有径向两亲结构的同多肽。 它们采用具有疏水螺旋芯和带电外壳的稳定的α-螺旋构象，由具有末端电荷基团的柔性疏水性侧链形成。 关于针对蛋白酶的稳定性和设计的简单性，径向两亲多肽提供了优于常规AMP的几个优点。 它们对革兰氏阴性菌和革兰氏阳性菌也具有较高的抗菌活性，溶血活性低。 因此，AMPs提供了用于治疗耐药细菌感染的通用平台。
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K38/00 | 含肽的医药配制品 |