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Ther Deliv. 2013 Jul;4(7):791-809. doi: 10.4155/tde.13.47.

Oligonucleotide conjugates for therapeutic applications.

Author information

1
Department of Medicinal Chemistry, University of Vienna, Vienna, Austria. johannes.winkler@univie.ac.at

Abstract

Insufficient pharmacokinetic properties and poor cellular uptake are the main hurdles for successful therapeutic development of oligonucleotide agents. The covalent attachment of various ligands designed to influence the biodistribution and cellular uptake or for targeting specific tissues is an attractive possibility to advance therapeutic applications and to expand development options. In contrast to advanced formulations, which often consist of multiple reagents and are sensitive to a variety of preparation conditions, oligonucleotide conjugates are defined molecules, enabling structure-based analytics and quality control techniques. This review gives an overview of current developments of oligonucleotide conjugates for therapeutic applications. Attached ligands comprise peptides, proteins, carbohydrates, aptamers and small molecules, including cholesterol, tocopherol and folic acid. Important linkage types and conjugation methods are summarized. The distinct ligands directly influence biochemical parameters, uptake mechanisms and pharmacokinetic properties.

PMID:
23883124
PMCID:
PMC3787477
DOI:
10.4155/tde.13.47
[Indexed for MEDLINE]
Free PMC Article
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