ArticleScientific reports2019
Extracellular and intracellular small-molecule galectin-3 inhibitors.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
48 citing papers in PubMed, 104 citations in OpenAlex.
- Safety and pharmacokinetics of GB1211, an oral galectin-3 inhibitor: a single- and multiple-dose first-in-human study in healthy participants.Cancer chemotherapy and pharmacology · 2023Trial
- Expression, Localization and Actions of Galectin-3: Implications in the Pathophysiology and Therapy of Cardiovascular Disease.International journal of molecular sciences · 2026Review
- Neurotrophins and Galectin-3: Hidden Keys in Neuroinflammation-A Narrative Review.International journal of molecular sciences · 2026Review
- Spatial N-glycan rearrangement on αNature communications · 2025Article
- Structural Insights Into Galectin-3 Recognition of a Selenoglycomimetic.ChemMedChem · 2025Article
- Rescue of mitochondrial dysfunction through alteration of extracellular matrix composition in barth syndrome cardiac fibroblasts.Biomaterials · 2025Article
- Uptake of small extracellular vesicles by recipient cells is facilitated by paracrine adhesion signaling.Nature communications · 2025Article
- Growth factor-triggered de-sialylation controls glycolipid-lectin-driven endocytosis.Nature cell biology · 2025Article
- Kinetic and Mechanistic Release Studies on Hyaluronan Hydrogels for Their Potential Use as a pH-Responsive Drug Delivery Device.Gels (Basel, Switzerland) · 2024Article
- Exploration into Galectin-3 Driven Endocytosis and Lattices.Biomolecules · 2024Article
- Lysosome quality control in health and neurodegenerative diseases.Cellular & molecular biology letters · 2024Review
- Identification of an H-Ras nanocluster disrupting peptide.Communications biology · 2024Article
- Endocytic Roles of Glycans on Proteins and Lipids.Cold Spring Harbor perspectives in biology · 2024Review
- Ligand Sulfur Oxidation State Progressively Alters Galectin-3-Ligand Complex Conformations To Induce Affinity-Influencing Hydrogen Bonds.Journal of medicinal chemistry · 2023Article
- The role of galectins in immunity and infection.Nature reviews. Immunology · 2023Review
- Galectin-3 inhibition as a potential therapeutic target in non-alcoholic steatohepatitis liver fibrosis.World journal of hepatology · 2023Review
- Targeting galectin-3 to counteract spike-phase uncoupling of fast-spiking interneurons to gamma oscillations in Alzheimer's disease.Translational neurodegeneration · 2023Article
- Targeting intracellular galectins for cancer treatment.Frontiers in immunology · 2023Review
- A new animal product free defined medium for 2D and 3D culturing of normal and cancer cells to study cell proliferation and migration as well as dose response to chemical treatment.Toxicology reports · 2023Article
- Immunomodulation exerted by galectins: a land of opportunity in rare cancers.Frontiers in immunology · 2023Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Galectin-3 is a carbohydrate binding protein which has important roles in cancer and immunity. Potent galectin-3 inhibitors have been synthesized, for experimental purposes and potential clinical use. As galectin-3 is implicated in both intra- and extracellular activities, permeability of galectin-3 inhibitors is an important parameter determining biological effects. We compared the cellular uptake of galectin-3 inhibitors and their potency in the intracellular or extracellular space. The inhibitors differed in their polar surface area (PSA), but had similar affinities for galectin-3. Using a well-established permeability assay, we confirmed that the uptake was significantly higher for the inhibitor with the lowest PSA, as expected. To analyze intracellular activity of the inhibitors, we developed a novel assay based on galectin-3 accumulation around damaged intracellular vesicles. The results show striking differences between the inhibitors intracellular potency, correlating with their PSAs. To test extracellular activity of the inhibitors, we analyzed their potency to block binding of galectin-3 to cell surfaces. All inhibitors were equally able to block galectin-3 binding to cells and this was proportional to their affinity for galectin-3. These inhibitors may serve as useful tools in exploring biological roles of galectin-3 and may further our understanding of intracellular versus extracellular roles of galectin-3.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.