Synthesis of Monovalent N‐Acetylgalactosamine Phosphoramidite for Liver‐Targeting Oligonucleotides
Sign Up to like & getrecommendations! Published in 2019 at "Current Protocols in Nucleic Acid Chemistry"
DOI: 10.1002/cpnc.99
Abstract: Ligand‐targeted drug delivery (LTDD) has emerged as an attractive option in the field of oligonucleotide drugs following the great success of N‐acetylgalactosamine (GalNAc)–conjugated siRNA and antisense oligonucleotides. GalNAc is a well‐known ligand of the asialoglycoprotein… read more here.
Keywords: acetylgalactosamine; galnac; moiety; monovalent ... See more keywords
In vitro synthesis of mucin-type O-glycans using saccharide primers comprising GalNAc-Ser and GalNAc-Thr residues.
Sign Up to like & getrecommendations! Published in 2021 at "Carbohydrate research"
DOI: 10.1016/j.carres.2021.108495
Abstract: Mucin-type O-glycosylation of serine or threonine residue in proteins is known to be one of the major post-translational modifications. In this study, two novel alkyl glycosides, Nα-lauryl-O-(2-acetamido-2-deoxy-α-d-galactopyranosyl)-l-serineamide (GalNAc-Ser-C12) and Nα-lauryl-O-(2-acetamido-2-deoxy-α-d-galactopyranosyl)-l-threonineamide (GalNAc-Thr-C12) were synthesized as saccharide… read more here.
Keywords: galnac; galnac ser; saccharide primers; mucin type ... See more keywords
GalNAc bio‐functionalization of nanoparticles assembled by electrostatic interactions improves siRNA targeting to the liver
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Controlled Release"
DOI: 10.1016/j.jconrel.2017.10.001
Abstract: ABSTRACT RNA interference (RNAi) has the potential to reversibly silence any gene with high efficiency and specificity. To fulfill the clinical potential of RNAi, delivery vehicles are required to transport the short interfering RNA (siRNA)… read more here.
Keywords: surface; functionalization nanoparticles; bio functionalization; galnac ... See more keywords
Differential Protein Precipitation-Based GalNAc-siRNA Sample Preparation with LC/MS Method Development Workflow in Plasma
Sign Up to like & getrecommendations! Published in 2025 at "Analytical Chemistry"
DOI: 10.1021/acs.analchem.5c01587
Abstract: Liquid chromatography–mass spectrometry (LC/MS) plays a crucial role in the quantification of small interfering RNAs (siRNAs) in biological matrices. However, the recovery of siRNA from complex biological matrices remains a significant challenge. Focusing on liver-targeted… read more here.
Keywords: method; protein precipitation; differential protein; galnac sirna ... See more keywords
Metabolically Stable Anomeric Linkages Containing GalNAc-siRNA Conjugates: An Interplay among ASGPR, Glycosidase, and RISC Pathways.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01337
Abstract: Conjugation of synthetic triantennary N-acetyl-d-galactosamine (GalNAc) to small interfering RNA (siRNA) mediates binding to the asialoglycoprotein receptor (ASGPR) on the surface of hepatocytes, facilitating liver-specific uptake and siRNA-mediated gene silencing. The natural β-glycosidic bond of… read more here.
Keywords: anomeric linkages; sirna; galnac sirna; glycosidase ... See more keywords
A Soluble Triantennary N-Acetylgalactosamine Camptothecin Prodrug for Hepatocellular Carcinoma-Targeted Therapy.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00466
Abstract: Camptothecin (CPT) and its derivatives are potent anticancer agents, but their clinical application is limited by poor aqueous solubility, lack of targeting specificity, and severe systemic toxicity. In this study, we synthesized a glycoconjugate prodrug,… read more here.
Keywords: cpt; triantennary acetylgalactosamine; hepatocellular carcinoma; galnac ... See more keywords
Detecting Glucose Fluctuations in the Campylobacter jejuni N-Glycan Structure.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical biology"
DOI: 10.1021/acschembio.1c00498
Abstract: Campylobacter jejuni is a significant cause of human gastroenteritis worldwide, and all strains express an N-glycan that is added to at least 80 different proteins. We characterized 98 C. jejuni isolates from infants from 7… read more here.
Keywords: campylobacter jejuni; detecting glucose; glucose fluctuations; galnac galnac ... See more keywords
Development of a GalNAc-Tyrosine-Specific Monoclonal Antibody and Detection of Tyrosine O-GalNAcylation in Numerous Human Tissues and Cell Lines.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c04477
Abstract: Glycosylation is a vital post-translational modification involved in a range of biological processes including protein folding, signaling, and cell-cell interactions. In 2011, a new type of O-linked glycosylation was discovered, wherein the side-chain oxygen of… read more here.
Keywords: tyrosine; cell; galnac; galnac tyr ... See more keywords
The structure of the colorectal cancer-associated enzyme GalNAc-T12 reveals how nonconserved residues dictate its function
Sign Up to like & getrecommendations! Published in 2019 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1902211116
Abstract: Significance While it is well established that heavily O-glycosylated mucins are essential for normal gastrointestinal function, it is not known how polypeptide N-acetylgalactosaminyl transferase (GalNAc-T12)–specific O-glycans may be contributing. Here we use structural, computational, and… read more here.
Keywords: galnac t12; function; colorectal cancer; galnac ... See more keywords
The Nonclinical Safety Profile of GalNAc-conjugated RNAi Therapeutics in Subacute Studies
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DOI: 10.1177/0192623318792537
Abstract: Short interfering RNAs (siRNAs) and antisense oligonucleotides (ASOs) are the most clinically advanced oligonucleotide-based platforms. A number of N-acetylgalactosamine (GalNAc)-conjugated siRNAs (GalNAc-siRNAs), also referred to as RNA interference (RNAi) therapeutics, are currently in various stages… read more here.
Keywords: rnai therapeutics; galnac conjugated; safety; galnac sirnas ... See more keywords
The GalNAc-T Activation Pathway (GALA) is not a general mechanism for regulating mucin-type O-glycosylation
Sign Up to like & getrecommendations! Published in 2017 at "PLoS ONE"
DOI: 10.1371/journal.pone.0179241
Abstract: Mucin-type O-glycosylation is initiated by the UDP-GalNAc polypeptide:N-acetylgalactosaminyltransferase (GalNAc-T) family of enzymes. Their activity results in the GalNAc α1-O-Thr/Ser structure, termed the Tn antigen, which is further decorated with additional sugars. In neoplastic cells, the… read more here.
Keywords: golgi complex; mechanism; mucin type; type glycosylation ... See more keywords