Antisense oligonucleotides (ASOs) conjugated to trivalent GalNAc ligands show 10-fold
enhanced potency for suppressing gene targets expressed in hepatocytes. Trivalent GalNAc …

Triantennary N-acetyl galactosamine (GalNAc, GN3), a high-affinity ligand for the hepatocyte-
specific asialoglycoprotein receptor (ASGPR), enhances the potency of second-generation …

Conjugation of triantennary N-acetyl galactosamine (GalNAc) to oligonucleotide
therapeutics results in marked improvement in potency for reducing gene targets expressed …

Triantennary N-acetyl galactosamine (GalNAc 3) is a high-affinity ligand for hepatocyte-
specific asialoglycoprotein receptors. Conjugation with GalNAc 3 via a trishexylamino (THA) …

The comprehensive structure–activity relationships of triantennary GalNAc conjugated ASOs
for enhancing potency via ASGR mediated delivery to hepatocytes is reported. Seventeen …

Targeted delivery of antisense oligonucleotides (ASO) to hepatocytes via the
asialoglycoprotein receptor (ASGR) has improved the potency of ASO drugs∼ 30-fold in the …

Antisense oligonucleotides (ASOs) are a novel therapeutic approach to target difficult-to-
drug protein classes by targeting their corresponding mRNAs. Significantly enhanced ASO …

The targeting of abundant hepatic asialoglycoprotein receptors (ASGPR) with trivalent N-
acetylgalactosamine (GalNAc) is a reliable strategy for efficiently delivering antisense …

The potency of antisense oligonucleotide (ASO) drugs has significantly improved in the
clinic after exploiting asialoglycoprotein receptor (ASGR) mediated delivery to hepatocytes …

Introduction: Triantennary N-acetyl galactosamine (GalNAc3)–conjugated antisense
oligonucleotides (ASOs) have demonstrated improved hepatocyte uptake and …