Cholesterol–GalNAc Dual Conjugation Strategy for Reducing Renal Distribution of Antisense Oligonucleotides

Recently, some studies have reported nephrotoxicity associated with a certain class of antisense oligonucleotides (ASOs) in humans. One possibility for reducing the potential nephrotoxicity of ASOs is to alter their pharmacokinetics. In this study, we investigated the effect of a ligand conjugation...

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Veröffentlicht in:	Nucleic acid therapeutics 2018-02, Vol.28 (1), p.5-57
Hauptverfasser:	Wada, Fumito, Yamamoto, Tsuyoshi, Ueda, Tetsuya, Sawamura, Motoki, Wada, Shunsuke, Harada-Shiba, Mariko, Obika, Satoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylgalactosamine - chemistry Acids Animals Antisense oligonucleotides Apolipoproteins B - antagonists & inhibitors Apolipoproteins B - genetics Apolipoproteins B - metabolism Asialoglycoprotein Receptor - genetics Asialoglycoprotein Receptor - metabolism Brief Communications Carbohydrate Sequence Cholesterol Cholesterol - chemistry Conjugation Drug dosages Gene Silencing Kidney - metabolism Kidneys Ligands Liver Liver - metabolism Liver diseases Male Mice Mice, Inbred C57BL N-Acetylgalactosamine Oligonucleotides Oligonucleotides, Antisense - chemistry Oligonucleotides, Antisense - genetics Oligonucleotides, Antisense - pharmacokinetics Pharmaceutical sciences Pharmacokinetics Pharmacology Protein Binding Research centers Strategy Tissue Distribution Toxicity
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