ArticleThrombosis research2015
Allosteric inhibition of factor XIa. Sulfated non-saccharide glycosaminoglycan mimetics as promising anticoagulants.
Article in Thrombosis research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 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.
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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
30 citing papers in PubMed, 44 citations in OpenAlex.
- Chemical Synthesis and Biochemical Evaluation of Decasulfated Galloylglucopyranose Heparin Mimetic.Cardiovascular & hematological agents in medicinal chemistry · 2026Article
- A one-step chemical derivatization strategy for mass spectrometric characterization of synthetic mimetics of sulfated glycosaminoglycans.Analytical methods : advancing methods and applications · 2026Article
- The Discovery of a Novel Anticoagulant Mechanism: Factor XI Activation Inhibitors.ACS pharmacology & translational science · 2025Article
- Emerging Targets, Novel Directions, and Innovative Approaches in Thrombosis Therapy.Aging and disease · 2025Review
- BIOCHEMICAL INVESTIGATION OF THE ANTICOAGULANT ACTIVITY OF SULFONATED POLYMERS.Journal of undergraduate chemistry research · 2025Article
- Sulfonated Penta-galloyl Glucose (SPGG): The Pharmacological Effects of Promiscuous Glycosaminoglycan Small Molecule Mimetic.Mini reviews in medicinal chemistry · 2025Review
- Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2024Article
- Triple Action of Lignosulfonic Acid Sodium: Anti-protease, Antioxidant, and Anti-inflammatory Effects of a Polymeric Heparin Mimetic.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2024Article
- Investigation of the anticoagulant activity of cyclic sulfated glycosaminoglycan mimetics.Carbohydrate research · 2023Article
- Glycated albumin modulates the contact system with implications for the kallikrein-kinin and intrinsic coagulation systems.Journal of thrombosis and haemostasis : JTH · 2023Article
- Sulphated penta-galloyl glucopyranoside (SPGG) is glycosaminoglycan mimetic allosteric inhibitor of cathepsin G.RPS pharmacy and pharmacology reports · 2023Article
- Factor XI/XIa Inhibition: The Arsenal in Development for a New Therapeutic Target in Cardio- and Cerebrovascular Disease.Journal of cardiovascular development and disease · 2022Review
- Sulfonated non-saccharide molecules and human factor XIa: Enzyme inhibition and computational studies.Chemical biology & drug design · 2022Article
- Murine Models in the Evaluation of Heparan Sulfate-Based Anticoagulants.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Factor XI, a potential target for anticoagulation therapy for venous thromboembolism.Frontiers in cardiovascular medicine · 2022Review
- Lignosulfonic Acid Sodium Is a Noncompetitive Inhibitor of Human Factor XIa.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Sulfated Oligomers of Tyrosol: Toward a New Class of Bioinspired Nonsaccharidic Anticoagulants.Biomacromolecules · 2021Article
- Discovery of Benzyl Tetraphosphonate Derivative as Inhibitor of Human Factor Xia.ChemistryOpen · 2020Article
- Article
- Sulfated Non-Saccharide Glycosaminoglycan Mimetics as Novel Drug Discovery Platform for Various Pathologies.Current medicinal chemistry · 2020Review
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3 authors at 1 institution in 1 country.
Funding
Abstract
Recent development of sulfated non-saccharide glycosaminoglycan mimetics, especially sulfated pentagalloyl glucopyranoside (SPGG), as potent inhibitors of factor XIa (FXIa) (J. Med. Chem. 2013; 56:867-878 and J. Med. Chem. 2014; 57:4805-4818) has led to a strong possibility of developing a new line of factor XIa-based anticoagulants. In fact, SPGG represents the first synthetic, small molecule inhibitor that appears to bind in site remote from the active site. Considering that allosteric inhibition of FXIa is a new mechanism for developing a distinct line of anticoagulants, we have studied SPGG's interaction with FXIa with a goal of evaluating its pre-clinical relevance. Comparative inhibition studies with several glycosaminoglycans revealed the importance of SPGG's non-saccharide backbone. SPGG did not affect the activity of plasma kallikrein, activated protein C and factor XIIIa suggesting that SPGG-based anticoagulation is unlikely to affect other pathways connected with coagulation factors. SPGG's effect on APTT of citrated human plasma was also not dependent on antithrombin or heparin cofactor II. Interestingly, SPGG's anticoagulant potential was diminished by serum albumin as well as factor XI, while it could be reversed by protamine or polybrene, which implies possible avenues for developing antidote strategy. Studies with FXIa mutants indicated that SPGG engages Lys529, Arg530 and Arg532, but not Arg250, Lys252, Lys253 and Lys255. Finally, SPGG competes with unfractionated heparin, but not with polyphosphates and/or glycoprotein Ibα, for binding to FXIa. These studies enhance understanding on the first allosteric inhibitor of FXIa and highlight its value as a promising anticoagulant.
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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.