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Nucleosides and Nucleotides Volume 16, 1997 - Issue 7-9
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III. PRECLINICAL STUDIES OF OLIGOMERS

Conjugation of Oligonucleotides with Steroid Structures and Their Interaction with the Low-Density Lipoprotein

Erik T. Rump Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9503, 2300, RA, Leiden, The Netherlands
,
Remco L.A. de Vrueh Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9503, 2300, RA, Leiden, The Netherlands
,
Erik A.L. Biessen Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9503, 2300, RA, Leiden, The Netherlands
,
Theo J.C. van Berkel Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9503, 2300, RA, Leiden, The Netherlands
&
Martin K. Bijsterbosch Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O. Box 9503, 2300, RA, Leiden, The Netherlands
Pages 1223-1226 | Published online: 16 Aug 2006
 
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Abstract

To induce association with low-density lipoprotein (LDL), antisense oligonucleotides were derivatized at their 3′ terminus with several steroid structures. It was found that only highly lipidic steroids can complex the oligonucleotide with LDL.

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