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Glycocluster Design...
Glycocluster Design for Improved Avidity and Selectivity in Blocking Human Lectin/Plant Toxin Binding to Glycoproteins and Cells
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- Andre, Sabine (författare)
- Univ Munich, Inst Physiol Chem, Tierarztliche Fak, D-80539 Munich, Germany.
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- Lahmann, Martina (författare)
- Univ Bangor, Sch Chem, Bangor LL57 2UW, Gwynedd, Wales.
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- Gabius, Hans-Joachim (författare)
- Univ Munich, Inst Physiol Chem, Tierarztliche Fak, D-80539 Munich, Germany.
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- Oscarson, Stefan (författare)
- Univ Coll Dublin, Ctr Synth & Chem Biol, Dublin 4, Ireland.
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Univ Munich, Inst Physiol Chem, Tierarztliche Fak, D-80539 Munich, Germany Univ Bangor, Sch Chem, Bangor LL57 2UW, Gwynedd, Wales. (creator_code:org_t)
- 2010-11-12
- 2010
- Engelska.
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Ingår i: Molecular Pharmaceutics. - : American Chemical Society (ACS). - 1543-8384 .- 1543-8392. ; 7:6, s. 2270-2279
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Blocking lectin/toxin binding to human cells by suitable inhibitors can therapeutically protect them from harmful effects. Clustered design of ligand presentation holds the promise of affinity increase relative to the free sugar and inherent selectivity among lectin targets. Using first a solid-phase assay with a glycoprotein presenting N-glycans as lectin-reactive probe, we assessed the inhibitory potency of bi- to tetravalent clusters on a plant toxin and three human adhesion/growth-regulatory lectins. Enhanced avidity relative to the free sugar was detected together with lectin-type selectivity. These effects were confirmed on the level of cells in vitro, also for two leguminous lectins. The lack of toxicity in cell proliferation assays excluded concerns to further work on these compounds. The given cluster design and the strategic combination of the two assay systems of increasing biorelevance will thus be helpful to take the next steps in drug development, e.g. tailoring the sugar headgroup.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Nyckelord
- Agglutinin
- colon cancer
- glycan branching
- glycocluster
- multivalency
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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