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    • 10. 发明申请
    • ANTIPATHOGENIC PEPTIDES AND COMPOSITIONS COMPRISING THEM
    • 抗病毒肽及其组合物
    • WO9731019A2
    • 1997-08-28
    • PCT/IL9700066
    • 1997-02-20
    • YEDA RES & DEVSHAI YECHIELOREN ZIV
    • SHAI YECHIELOREN ZIV
    • A61K38/00A61K31/00A61K38/04A61K38/17A61P31/00A61P31/04A61P31/10A61P31/12A61P33/00A61P35/00C07K20060101C07K14/00C07K14/435C07K14/46
    • C07K14/461A61K38/00C07K14/001C07K14/43572
    • Peptides which have a net positive charge and none or only a partial alpha -helix configuration were found to have a non-hemolytic selective cytolytic activity. The peptides may be derived from natural peptides such as pardaxin and mellitin and fragments thereof in which L-amino acid residues are replaced by corresponding D-amino acid residues, and cyclic derivatives of the foregoing, or are diastereomers of linear peptides composed of varying ratios of at least one positively charged amino acid and at least one hydrophobic amino acid, and in which at least one of the amino acid residues is a D-amino acid, and preferably at least one third of the sequence is composed of D-amino acid residues. Pharmaceutical compositions comprising the non-hemolytic cytolytic peptides can be used for the treatment of several diseases caused by pathogens including antibacterial, fungal, viral, mycoplasma and protozoan infections and for the treatment of cancer.
    • 发现具有净正电荷且没有或仅部分α-螺旋构型的肽具有非溶血性选择性溶细胞活性。 肽可以衍生自其中L-氨基酸残基被相应的D-氨基酸残基替代的天然肽,例如泛珠蛋白和麦角蛋白及其片段,以及前述的环状衍生物,或者是由不同比例组成的线性肽的非对映异构体 的至少一个带正电荷的氨基酸和至少一个疏水性氨基酸,并且其中至少一个氨基酸残基是D-氨基酸,并且优选该序列的至少三分之一由D-氨基酸组成 残留物。 包含非溶血性溶细胞肽的药物组合物可用于治疗由包括抗菌,真菌,病毒,支原体和原生动物感染在内的病原体引起的几种疾病和用于治疗癌症。