Download the GalNAc Ligands Product Brochure (2022)

Exploiting GalNAc in receptor-mediated drug delivery through use of glycobiology offers a means of addressing the specific challenge of delivering and targeting therapeutic molecules such as proteins, antibodies and oligonucleotides. The idea that carbohydrates, including GalNAc, mediate receptor binding, cell targeting and cellular uptake of molecules has been been known for decades. The Ashwell–Morell receptors found in liver hepatocytes, originally and more commonly referred to as the asialoglycoprotein receptor (ASGPR), was the first lectin to be detected in mammals and the first cellular receptor to be identified and isolated. It is one of the multiple lectins of the C-type lectin family involved in recognition, binding, and clearance of asialo glycoproteins. GalNAc has been adopted and successfully applied as a targeting ligand in antisense oligonucleotides and siRNA guiding therapeutic payloads into liver cells. Cell-specific delivery of therapeutic agents via ASGPR using GalNAc ligands offers incredible potential.

Sussex Research Laboratories Inc. has developed an extensive selection of functionalized GalNAc ligands with various alkyl and/or polyethylene glycol (PEG) linker/spacer systems. These enable facile introduction of GalNAc-based recognition elements onto a variety of molecules including but not limited to small molecules, surfaces, nanoparticles, peptides, proteins, antibodies, lipids and oligonucleotides.

Various functionalized GalNAc ligands include:

1. DBCO (dibenzocyclooctyne) – react with azides via copperless click chemistry
2. Alkynes – react with azides via copper-catalyzed click chemistry
3. Azides – react with triple bonds via click chemistry
4. Maleimides – react with thiols
5. Amines – react with carboxylic acids
6. Carboxylic acids – amine reactive
7. NHS esters (including sulfo-NHS esters) – amine reactive
8. Pentafluorophenolic esters – amine reactive
9. Controlled Pore Glass (CPG)
10. Biotin – for detection of tris-GalNAc ligands via streptavidin
11. Fluorescein – for detection of tris-GalNAc ligands
12. Lipids – preparation of targeted nanoparticles
13. Alkyl and discrete, monodisperse polyethylene glycols (PEGS)
14. Polydisperse polyethylene glycols (PEGS)

View our GalNAc ligand listing below. If you’re unable to find what you’re looking for, please request for a custom synthesis.