ReviewBioorganic & medicinal chemistry2023
Discovery and development of small-molecule heparanase inhibitors.
Review in Bioorganic & medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 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
10 citing papers in PubMed.
- Chitosan Oligosaccharides Modulate Macrophage Inflammatory Signaling: Molecular Docking and Transcriptomic Evidence.International journal of molecular sciences · 2026Article
- Machine learning based approaches for structure activity relationship analysis of heparanase inhibitors.Scientific reports · 2026Article
- Effect of alprostadil combined with sulodexide on elderly chronic kidney disease patients and the independent risk factors affecting curative results.American journal of translational research · 2026Article
- From Native Glycosaminoglycans to Mimetics: Design, Mechanisms, and Biomedical Applications.Biomolecules · 2025Review
- From Docking and Molecular Dynamics to Experimental Discovery: Exploring the Hydrophobic Landscapes of Heparanase to Design Potent Inhibitors.Journal of chemical information and modeling · 2025Article
- A Novel Series of Synthetic Heparin-Mimetics-Itaconic Acid-Containing Copolymers for Targeting Tumor Cell Coagulability and Metastasis.Macromolecular bioscience · 2025Article
- Design of Paromomycin and Neomycin as Sulfated and Hydrophobic Glycans to Target Heparanase-Driven Tumor Progression and Metastasis.Journal of medicinal chemistry · 2025Article
- Maculopathy after long-term use of fondaparinux, a heparin mimetic and heparanase inhibitor.American journal of ophthalmology case reports · 2025Article
- The Model of Neutrophil Chemotaxis Participated by the Vascular Endothelial Glycocalyx.International journal of general medicine · 2025Review
- Design Principle of Heparanase Inhibitors: A Combined In Vitro and In Silico Study.ACS medicinal chemistry letters · 2024Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Heparanase-1 (HPSE) is a promising yet challenging therapeutic target. It is the only known enzyme that is responsible for cleavage of heparan sulfate (HS) side chains from heparan sulfate proteoglycans (HSPGs), and is the key enzyme involved in the remodeling and degradation of the extracellular matrix (ECM). Overexpression of HPSE is found in various types of diseases, including cancers, inflammations, diabetes, and viral infections. Inhibiting HPSE can restore ECM functions and integrity, making the development of HPSE inhibitors a highly sought-after topic. So far, all HPSE inhibitors that have entered clinical trials belong to the category of HS mimetics, and no small-molecule or drug-like HPSE inhibitors have made similar progress. None of the HS mimetics have been approved as drugs, with some clinical trials discontinued due to poor bioavailability, side effects, and unfavorable pharmacokinetics characteristics. Small-molecule HPSE inhibitors are, therefore, particularly appealing due to their drug-like characteristics. Advances in the chemical spaces and drug design technologies, including the increasing use of in vitro and in silico screening methods, have provided new opportunities in drug discovery. This article aims to review the discovery and development of small-molecule HPSE inhibitors via screening strategies to shed light on the future endeavors in the development of novel HPSE inhibitors.
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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.