Lipophilic polynucleotide conjugates

Details Lipophilic polynucleotide conjugates Lipophilic polynucleotide conjugates

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) A61K 47/48 (2006.01) C12N 15/87 (2006.01) C07J 9/00 (2006.01)

Patent

CA 2761106

Disclosed are lipophilic polynucleotide conjugates including polynucleotide-cholesterol conjugates and methods of delivering therapeutic polynucleotides to a mammalian cell or patient in need of treatment using said conjugates. The disclosure further provides methods of synthesizing the lipophilic polynucleotide conjugates.The conjugates are designed to mimic or target cellular miRNAs. The lipophilic moiety, such as cholesterol or cholesterol derivative, is spaced from the polynucleotide by a substantially linear hydrocarbon group. Due to an absence of significantly polar groups and/or exchangeable protons in the vicinity of the lipophilic moiety, the interaction between the lipophilic moiety and cell membranes is enhanced to provide for efficient entry into cells.

Cette invention concerne des conjugués polynucléotidiques lipophiles comprenant des conjugués polynucléotide-cholestérol et des méthodes d'introduction de polynucléotidiques thérapeutiques dans une cellule de mammifère ou chez un mammifère ayant besoin d'un traitement au moyen desdits conjugués. L'invention concerne par ailleurs des méthodes de synthèse de ces conjugués polynucléotidiques lipophiles. Selon l'invention, les conjugués sont conçus pour imiter ou cibler les micro-ARN cellulaires. La fraction lipophile, par exemple le cholestérol ou un dérivé du cholestérol, est séparée du polynucléotide par un groupe hydrocarboné sensiblement linéaire. L'absence de groupes significativement polaires et/ou de protons échangeables à proximité de la fraction lipophile permet d'améliorer l'interaction entre la fraction lipophile et les membranes cellulaires, et assure ainsi la pénétration efficace du conjugué dans les cellules.

Affiliated with

Also associated with

Rating

Lipophilic polynucleotide conjugates does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Lipophilic polynucleotide conjugates, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Lipophilic polynucleotide conjugates will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1472400