Abstract
This review summarizes the effect of conjugating small molecules and large biomacromolecules to antisense oligonucleotides to improve their therapeutic potential. In many cases, favorable changes in pharmacokinetic and pharmacodynamic properties were observed. Opportunities exist to change the terminating mechanism of antisense action or to enhance the RNase H mode of action via conjugate formation.
MeSH terms
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Animals
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Biological Transport, Active
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Carbohydrates
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Cations
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Cholesterol
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Cross-Linking Reagents
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Endocytosis
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Humans
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Ligands
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Liver / drug effects
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Liver / metabolism
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Oligonucleotides, Antisense / chemistry
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Oligonucleotides, Antisense / pharmacokinetics*
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Oligonucleotides, Antisense / pharmacology*
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Polyethylene Glycols
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Porphyrins
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Protein Binding
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Ribonuclease H / metabolism
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Tissue Distribution
Substances
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Carbohydrates
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Cations
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Cross-Linking Reagents
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Ligands
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Oligonucleotides, Antisense
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Porphyrins
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Polyethylene Glycols
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Cholesterol
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Ribonuclease H