公开(公告)号：US20070135333A1

公开(公告)日：2007-06-14

申请号：US11487009

申请日：2006-07-13

申请人： Bruce Geller ,  Patrick Iversen ,  Lucas Tilley

发明人： Bruce Geller ,  Patrick Iversen ,  Lucas Tilley

IPC分类号： A61K48/00

CPC分类号： A61K48/00 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/3233 ,  C12N2310/3513 ,  C12N2320/50

摘要： An antibacterial antisense conjugate and method of using the same for treating a bacterial infection in a mammalian host are disclosed. The conjugate includes an antisense oligonucleotide conjugated to a carrier peptide that significantly enhances the antibacterial activity of the oligonucleotide. The antisense oligonucleotide contains 10-20 nucleotide bases and has a targeting nucleic acid sequence complementary to a target sequence containing or within 10 bases, in a downstream direction, of the translational start codon of a bacterial mRNA that encodes a bacterial protein essential for bacterial replication, where the compound binds to a target mRNA with a Tm of between 50° to 60° C. The carrier peptide is an arginine-rich peptide containing between 6 and 12 amino acids.

摘要翻译： 公开了一种抗菌反义结合物及其用于治疗哺乳动物宿主细菌感染的方法。 缀合物包括与载体肽缀合的反义寡核苷酸，其显着增强寡核苷酸的抗菌活性。 反义寡核苷酸含有10-20个核苷酸碱基，并且具有与含有或在其下游方向的10个碱基的靶序列互补的靶向核酸序列，其编码细菌复制物必需的细菌蛋白质的细菌mRNA的翻译起始密码子 其中化合物与50℃至60℃之间的T mRNA结合靶mRNA。载体肽是含有6至12个氨基酸的富含精氨酸的肽。