Antisense antibacterial method and compound

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01) C12N 15/113 (2010.01) A61P 31/04 (2006.01) C07H 21/04 (2006.01) A61K 31/7125 (2006.01)

Patent

CA 2614191

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 600C. The carrier peptide is an arginine-rich peptide containing between 6 and 12 amino acids.

L'invention concerne un conjugué antisens antibactérien et son procédé d'utilisation pour le traitement d'une infection bactérienne chez un hôte mammifère. Le conjugué comprend un oligonucléotide antisens conjugué à un peptide porteur qui accroît sensiblement l'activité antibactérienne de l'oligonucléotide. L'oligonucléotide antisens contient 10-20 bases nucléotidiques et possède une séquence nucléotidique de ciblage complémentaire d'une séquence cible contenant 10 bases ou comprise dans 10 bases, vers l'aval, du codon initiateur de traduction d'un ARNm bactérien qui code pour une protéine bactérienne essentielle pour la réplication bactérienne, le composé se liant à un ARNm cible à une Tm de 50 à 600 °C. Le peptide porteur est un peptide riche en arginine contenant entre 6 et 12 acides aminés.

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