Characterizing the effect of GalNAc and phosphorothioate backbone on binding of antisense oligonucleotides to the asialoglycoprotein receptor

Conjugation of mono and di-GalNAc sugars enhances the potency of antisense oligonucleotides via ASGR mediated delivery to hepatocytes

(2016) Garth A. Kinberger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Comprehensive Structure–Activity Relationship of Triantennary N-Acetylgalactosamine Conjugated Antisense Oligonucleotides for Targeted Delivery to Hepatocytes

(2016) Thazha P. Prakash et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antisense oligonucleotides targeting apolipoprotein(a) in people with raised lipoprotein(a): two randomised, double-blind, placebo-controlled, dose-ranging trials

(2016) Nicholas J Viney et al.   LANCET

Stabilin-1 and Stabilin-2 are specific receptors for the cellular internalization of phosphorothioate-modified antisense oligonucleotides (ASOs) in the liver

(2016) Colton M. Miller et al.   NUCLEIC ACIDS RESEARCH

siRNA Conjugates Carrying Sequentially Assembled Trivalent N-Acetylgalactosamine Linked Through Nucleosides Elicit Robust Gene Silencing In Vivo in Hepatocytes

(2015) Shigeo Matsuda et al.   ACS Chemical Biology

Efficient Synthesis and Biological Evaluation of 5′-GalNAc Conjugated Antisense Oligonucleotides

(2015) Michael E. Østergaard et al.   BIOCONJUGATE CHEMISTRY

Asialoglycoprotein receptor mediated hepatocyte targeting — Strategies and applications

(2015) Anisha A. D'Souza et al.   JOURNAL OF CONTROLLED RELEASE

DNA/RNA heteroduplex oligonucleotide for highly efficient gene silencing

(2015) Kazutaka Nishina et al.   Nature Communications

Multivalent N-Acetylgalactosamine-Conjugated siRNA Localizes in Hepatocytes and Elicits Robust RNAi-Mediated Gene Silencing

(2014) Jayaprakash K. Nair et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

TCP1 complex proteins interact with phosphorothioate oligonucleotides and can co-localize in oligonucleotide-induced nuclear bodies in mammalian cells

(2014) Xue-hai Liang et al.   NUCLEIC ACIDS RESEARCH

Targeted delivery of antisense oligonucleotides to hepatocytes using triantennaryN-acetyl galactosamine improves potency 10-fold in mice

(2014) Thazha P. Prakash et al.   NUCLEIC ACIDS RESEARCH

Liver as a target for oligonucleotide therapeutics

(2013) Alfica Sehgal et al.   JOURNAL OF HEPATOLOGY

Development of a fluorescence polarization binding assay for asialoglycoprotein receptor

(2012) Anna Y. Kornilova et al.   ANALYTICAL BIOCHEMISTRY

Clinical pharmacological properties of mipomersen (Kynamro), a second generation antisense inhibitor of apolipoprotein B

(2012) Stanley T. Crooke et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Glycomimetic Ligands for the Human Asialoglycoprotein Receptor

(2012) Sreeman K. Mamidyala et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

RNA Targeting Therapeutics: Molecular Mechanisms of Antisense Oligonucleotides as a Therapeutic Platform

(2010) C. Frank Bennett et al.   Annual Review of Pharmacology and Toxicology

Trivalent, Gal/GalNAc-containing ligands designed for the asialoglycoprotein receptor

(2008) Oleg Khorev et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The Asialoglycoprotein Receptor Regulates Levels of Plasma Glycoproteins Terminating with Sialic Acid α2,6-Galactose

(2008) Lindsay M. Steirer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY