CHOLIC-ACID OLIGONUCLEOTIDE CONJUGATES FOR ANTISENSE APPLICATIONS

Authors
MANOHARAN M JOHNSON LK BENNETT CF VICKERS TA ECKER DJ COWSERT LM FREIER SM COOK PD
Citation
M. Manoharan et al., CHOLIC-ACID OLIGONUCLEOTIDE CONJUGATES FOR ANTISENSE APPLICATIONS, Bioorganic & medicinal chemistry letters, 4(8), 1994, pp. 1053-1060
Citations number
29
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
8
Year of publication
1994
Pages
1053 - 1060
Database
ISI
SICI code
0960-894X(1994)4:8<1053:COCFAA>2.0.ZU;2-X
Abstract
To improve the pharmacokinetics of antisense oligonucleotides, cholic acid was conjugated to several biologically active sequences. Physical and biological properties of the conjugates were examined. While the cholic acid conjugation changes the lipophilicity of the oligonucleoti des, the in vitro biological activity observed was dependent on the di sease target, cell lines and the method of oligonucleotide treatment.