ArticleHistochemistry and cell biology2017
Teaming up synthetic chemistry and histochemistry for activity screening in galectin-directed inhibitor design.
Article in Histochemistry and cell biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Organoruthenium Glycomimetics Exhibit High Selectivity and Nanomolar Affinity for Human Galectin-1.Journal of medicinal chemistry · 2026Article
- Synthesis of the 3'-Beilstein journal of organic chemistry · 2024Article
- What is the Sugar Code?Chembiochem : a European journal of chemical biology · 2022Review
- In focus in HCB.Histochemistry and cell biology · 2021Article
- Recent Development in the Design of Neoglycoliposomes Bearing Arborescent Architectures.Molecules (Basel, Switzerland) · 2021Review
- Glycosylation in Axonal Guidance.International journal of molecular sciences · 2021Review
- Synthesis of Galectin Inhibitors by Regioselective 3'-Molecules (Basel, Switzerland) · 2020Article
- Influence of protein (human galectin-3) design on aspects of lectin activity.Histochemistry and cell biology · 2020Article
- How galectins have become multifunctional proteins.Histology and histopathology · 2020Review
- Revealing biomedically relevant cell and lectin type-dependent structure-activity profiles for glycoclusters by using tissue sections as an assay platform.RSC advances · 2018Article
- From glycophenotyping by (plant) lectin histochemistry to defining functionality of glycans by pairing with endogenous lectins.Histochemistry and cell biology · 2018Review
- Exploring functional pairing between surface glycoconjugates and human galectins using programmable glycodendrimersomes.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Article
- Studying the Structural Significance of Galectin Design by Playing a Modular Puzzle: Homodimer Generation from Human Tandem-Repeat-Type (Heterodimeric) Galectin-8 by Domain Shuffling.Molecules (Basel, Switzerland) · 2017Article
- Network analysis of adhesion/growth-regulatory galectins and their binding sites in adult chicken retina and choroid.Journal of anatomy · 2017Article
- Lipid glycosylation: a primer for histochemists and cell biologists.Histochemistry and cell biology · 2017Review
- Eukaryotic protein glycosylation: a primer for histochemists and cell biologists.Histochemistry and cell biology · 2017Review
- An introduction to the sugar code.Histochemistry and cell biology · 2017Article
- C-type lectins: their network and roles in pathogen recognition and immunity.Histochemistry and cell biology · 2017Review
- The sugar code in neuronal physiology.Histochemistry and cell biology · 2017Review
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A hallmark of endogenous lectins is their ability to select a few distinct glycoconjugates as counterreceptors for functional pairing from the natural abundance of cellular glycoproteins and glycolipids. As a consequence, assays to assess inhibition of lectin binding should necessarily come as close as possible to the physiological situation, to characterize an impact of a synthetic compound on biorelevant binding with pharmaceutical perspective. We here introduce in a proof-of-principle manner work with sections of paraffin-embedded tissue (jejunum, epididymis) and labeled adhesion/growth-regulatory galectins, harboring one (galectin-1 and galectin-3) or two (galectin-8) types of lectin domain. Six pairs of synthetic lactosides from tailoring of the headgroup (3'-O-sulfation) and the aglycone (β-methyl to aromatic S- and O-linked extensions) as well as three bi- to tetravalent glycoclusters were used as test compounds. Varying extents of reduction in staining intensity by synthetic compounds relative to unsubstituted/free lactose proved the applicability and sensitivity of the method. Flanking cytofluorimetric assays on lectin binding to native cells gave similar grading, excluding a major impact of tissue fixation. The experiments revealed cell/tissue binding of galectin-8 preferentially via one domain, depending on the cell type so that the effect of an inhibitor in a certain context cannot be extrapolated to other cells/tissues. Moreover, the work with the other galectins attests that this assay enables comprehensive analysis of the galectin network in serial tissue sections to determine overlaps and regional differences in inhibitory profiles.
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Registered trials
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