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Binding of synthetic oligosaccharides to the hepatic Gal/GalNAc lectin. Dependence on fine structural features.
Open accessAbstract
A series of synthetic oligosaccharides, resembling natural N-acetyllactosamine type glycans, were tested for their ability to inhibit the binding of labeled ligand to the mammalian hepatic lectin on rabbit hepatocytes at 2 degrees C. A dramatic hierarchy of inhibitory potency (tetraantennary greater than triantennary much greater than biantennary much greater than monoantennary) could be demonstrated. The range of concentration required for 50% inhibition of labeled ligand binding extended from approximately 1 mM, for the monoantennary oligosaccharides, to approximately 1 nM for triantennary oligosaccharides, even though the absolute Gal concentration increased only 3-fold. It was found that the number of Gal residues/cluster and their branching mode are major determinants of binding affinity of ligands to the hepatic lectin on the surface of hepatocytes.
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“A single subcutaneous injection of trivalent GalNAc-conjugated siRNA can achieve efficacy for >12 months22, 2324.”
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Rendle, P. M., Seger, A., Rodrigues, J. A., Oldham, N. J., Bott, R., Jones, J. B., Cowan, M. M., & Davis, B. G. (2004) · Journal of the American Chemical Society · doi:10.1021/ja031698u · Cited by 92
Metadata
- Authors
- Lee, Y. C., Townsend, R. R., Hardy, M. R., Lönngren, J., Arnarp, J., Haraldsson, M., & Lönn, H.
- Affiliations
- Johns Hopkins University (US)
- ORCID
- Haraldsson, M
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1983-01
- Volume
- 258
- Issue
- 1
- Pages
- 199-202
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1595570412
- Cited by
- 503
- References
- 24
- Citations by year
- 2026: 7 · 2025: 6 · 2024: 10 · 2023: 18 · 2022: 11 · 2021: 15 · 2020: 17 · 2019: 9 · 2018: 10 · 2017: 4 · 2016: 7 · 2015: 13 · 2014: 14 · 2013: 13 · 2012: 19
- FWCI
- 5.24
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Biological Chemistry (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Glycosylation and Glycoproteins Research
- Physical Sciences › Chemistry › Organic Chemistry › Carbohydrate Chemistry and Synthesis
- Life Sciences › Immunology and Microbiology › Immunology › Galectins and Cancer Biology
- Keywords
- Gal/GalNAc lectin, synthetic oligosaccharides, N-acetyllactosamine, oligosaccharide branching, hepatocytes
- MeSH terms
- Animals, Binding, Competitive, Carbohydrate Sequence, Cell Membrane, Glycopeptides, Kinetics, Liver, Oligosaccharides, Rabbits, Structure-Activity Relationship, Lectins
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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
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