Design and properties of hepatitis C virus antisense oligonucleotides for liver specific drug targeting.
Different backbone modified antisense oligonucleotides (AS-ODNs) directed against the hepatitis C virus genome were 5'-conjugated to cholesterol, cholic acid or taurocholic acid to enhance liver specific drug targeting and hepatocellular uptake. The lipophilic character of modified AS-ODNs was determined from RP-HPLC retention times and duplex stability was correlated with Tm-values from UV melting curves.
Lehmann
T J
TJ
Institute of Organic Chemistry, Johann Wolfgang Goethe-University, Marie-Curie-Strasse 11, D-60439 Frankfurt am Main, Germany.
Serwe
M
M
Caselmann
W H
WH
Engels
J W
JW
D002784:Cholesterol / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D019826:Cholic Acid / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D016174:Hepacivirus / Q000187:drug effects / Q000235:genetics*; D008099:Liver / Q000378:metabolism*; D016376:Oligonucleotides, Antisense / Q000737:chemistry* / Q000235:genetics* / Q000493:pharmacokinetics; D009928:Organ Specificity; D013656:Taurocholic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics
D016376:Oligonucleotides, Antisense; D013656:Taurocholic Acid; D002784:Cholesterol; D019826:Cholic Acid