ArticleFEBS open bio2013
Mechanisms of heparanase inhibition by the heparan sulfate mimetic PG545 and three structural analogues.
Article in FEBS open bio, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 59 citations in OpenAlex.
- Could Hydrophobicity of Sulfated Pseudo-Trisaccharides Derived from Repurposing Aminoglycoside Tobramycin Modulate the Enzymatic Activity of Heparanase?Journal of medicinal chemistry · 2025Article
- Heparanase-2 protein and peptides have a protective effect on experimental glomerulonephritis and diabetic nephropathy.Frontiers in pharmacology · 2023Article
- Review
- Structural Insights into Pixatimod (PG545) Inhibition of Heparanase, a Key Enzyme in Cancer and Viral Infections.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Identification and Repurposing of Trisubstituted Harmine Derivatives as Novel Inhibitors ofMolecules (Basel, Switzerland) · 2020Article
- The Heparan Sulfate Mimetic PG545 Modulates T Cell Responses and Prevents Delayed-Type Hypersensitivity.Frontiers in immunology · 2020Article
- Targeting Heparanase in Cancer: Inhibition by Synthetic, Chemically Modified, and Natural Compounds.iScience · 2019Review
- Glycosaminoglycans and Glycosaminoglycan Mimetics in Cancer and Inflammation.International journal of molecular sciences · 2019Review
- Heparanase: A Challenging Cancer Drug Target.Frontiers in oncology · 2019Review
- Leukocyte Heparanase: A Double-Edged Sword in Tumor Progression.Frontiers in oncology · 2019Review
- Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors.Journal for immunotherapy of cancer · 2018Article
- Heparin Mimetics: Their Therapeutic Potential.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Involvement of heparanase in the pathogenesis of acute kidney injury: nephroprotective effect of PG545.Oncotarget · 2017Article
- Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase.Glycobiology · 2016Article
- Heparan sulfate mimetic PG545-mediated antilymphoma effects require TLR9-dependent NK cell activation.The Journal of clinical investigation · 2016Article
- Structural characterization of human heparanase reveals insights into substrate recognition.Nature structural & molecular biology · 2015Article
- Molecular and clinical profiles of syndecan-1 in solid and hematological cancer for prognosis and precision medicine.Oncotarget · 2015Review
- The tumour microenvironment after radiotherapy: mechanisms of resistance and recurrence.Nature reviews. Cancer · 2015Review
- PG545 enhances anti-cancer activity of chemotherapy in ovarian models and increases surrogate biomarkers such as VEGF in preclinical and clinical plasma samples.European journal of cancer (Oxford, England : 1990) · 2015Article
- The Role of Heparanase and Sulfatases in the Modification of Heparan Sulfate Proteoglycans within the Tumor Microenvironment and Opportunities for Novel Cancer Therapeutics.Frontiers in oncology · 2014Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The tetrasaccharide heparan sulfate (HS) mimetic PG545, a clinical anti-cancer candidate, is an inhibitor of the HS-degrading enzyme heparanase. The kinetics of heparanase inhibition by PG545 and three structural analogues were investigated to understand their modes of inhibition. The cholestanol aglycon of PG545 significantly increased affinity for heparanase and also modified the inhibition mode. For the tetrasaccharides, competitive inhibition was modified to parabolic competition by the addition of the cholestanol aglycon. For the trisaccharides, partial competitive inhibition was modified to parabolic competition. A schematic model to explain these findings is presented.
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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.