Antimicrobial peptides and methods of use
    3.
    发明授权
    Antimicrobial peptides and methods of use 有权
    抗菌肽及其使用方法

    公开(公告)号:US08252737B2

    公开(公告)日:2012-08-28

    申请号:US11721915

    申请日:2005-12-15

    IPC分类号: A61K38/16

    CPC分类号: C07K14/4723 A61K38/00

    摘要: Disclosed herein are novel antimicrobial peptides with useful, improved, or superior properties such as antimicrobial activity, desirable levels of hemolytic activity, and therapeutic index against a broad range of microorganisms including gram-negative and gram-positive bacteria and other organisms having a cellular or structural component of a lipid bilayer membrane. Also provided are methods of making and using such peptides to control microbial growth and in pharmaceutical compositions for treatment or prevention of infections caused by such microorganisms. Certain peptides are disclosed utilizing a structure-based rational design relating to an antimicrobial peptide, V681, with single D-/L-amino acid substitutions or charged residue substitutions in or near the center of the peptide on the nonpolar or polar face. Also disclosed are peptides with one or more amino acids in the D configuration, including peptides with all amino acids in the D configuration. Modified peptide analogs herein can demonstrate one or more properties such as improved antimicrobial activity, specificity, and resistance to degradation. Compositions disclosed herein have useful clinical potential as antibiotics including broad spectrum antibiotics.

    摘要翻译: 本文公开了具有有用的,改进的或优异的性质的新型抗微生物肽,例如抗微生物活性,理想的溶血活性水平和针对广泛范围的微生物(包括革兰氏阴性和革兰氏阳性细菌和其他生物)的治疗指数,其具有细胞或 脂质双层膜的结构组分。 还提供了制备和使用这些肽来控制微生物生长的方法和用于治疗或预防由这种微生物引起的感染的药物组合物。 使用与抗微生物肽V681相关的基于结构的合理设计,在非极性或极性面上的肽中心附近具有单个D- / L-氨基酸置换或带电残基取代的某些肽被公开。 还公开了具有D构型中的一个或多个氨基酸的肽,包括具有D构型中所有氨基酸的肽。 本文中修饰的肽类似物可以证明一种或多种性质,例如改善的抗微生物活性,特异性和抗降解性。 本文公开的组合物作为抗生素包括广谱抗生素具有有用的临床潜力。

    Antimicrobial Peptides and Methods of Use
    4.
    发明申请
    Antimicrobial Peptides and Methods of Use 有权
    抗菌肽及其使用方法

    公开(公告)号:US20090005300A1

    公开(公告)日:2009-01-01

    申请号:US11721915

    申请日:2005-12-15

    CPC分类号: C07K14/4723 A61K38/00

    摘要: Disclosed herein are novel antimicrobial peptides with useful, improved, or superior properties such as antimicrobial activity, desirable levels of hemolytic activity, and therapeutic index against a broad range of microorganisms including gram-negative and gram-positive bacteria and other organisms having a cellular or structural component of a lipid bilayer membrane. Also provided are methods of making and using such peptides to control microbial growth and in pharmaceutical compositions for treatment or prevention of infections caused by such microorganisms. Certain peptides are disclosed utilizing a structure-based rational design relating to an antimicrobial peptide, V681, with single D-/L-amino acid substitutions or charged residue substitutions in or near the center of the peptide on the nonpolar or polar face. Also disclosed are peptides with one or more amino acids in the D configuration, including peptides with all amino acids in the D configuration. Modified peptide analogs herein can demonstrate one or more properties such as improved antimicrobial activity, specificity, and resistance to degradation. Compositions disclosed herein have useful clinical potential as antibiotics including broad spectrum antibiotics.

    摘要翻译: 本文公开了具有有用的,改进的或优异的性质的新型抗微生物肽,例如抗微生物活性,理想的溶血活性水平和针对广泛范围的微生物(包括革兰氏阴性和革兰氏阳性细菌和其他生物)的治疗指数,其具有细胞或 脂质双层膜的结构组分。 还提供了制备和使用这些肽来控制微生物生长的方法和用于治疗或预防由这种微生物引起的感染的药物组合物。 使用与抗微生物肽V681相关的基于结构的合理设计,在非极性或极性面上的肽中心附近具有单个D- / L-氨基酸置换或带电残基取代的某些肽被公开。 还公开了具有D构型中的一个或多个氨基酸的肽,包括具有D构型中所有氨基酸的肽。 本文中修饰的肽类似物可以证明一种或多种性质,例如改善的抗微生物活性,特异性和抗降解性。 本文公开的组合物作为抗生素包括广谱抗生素具有有用的临床潜力。