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Journal ArticleDOI

Structure-activity relationship in heparin : a synthetic pentasaccharide with high affinity for antithrombin III and eliciting high anti-factor Xa activity

TLDR
Results confirm that the synthetic pentasaccharide with the above structure corresponds to the actual minimal sequence required in heparin for binding to AT-III.
About
This article is published in Biochemical and Biophysical Research Communications.The article was published on 1983-10-31. It has received 640 citations till now. The article focuses on the topics: Tetrasaccharide.

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Citations
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Heparin-protein interactions

TL;DR: This review focuses on aspects of heparin structure and conformation, which are important for its interactions with proteins, and describes the interaction ofheparin and heparan sulfate with selected families of heParin-binding proteins.
Journal ArticleDOI

How were new medicines discovered

TL;DR: It is postulate that a target-centric approach for first-in-class drugs, without consideration of an optimal MMOA, may contribute to the current high attrition rates and low productivity in pharmaceutical research and development.
Journal ArticleDOI

Heparin and Low-Molecular-Weight Heparin Mechanisms of Action, Pharmacokinetics, Dosing, Monitoring, Efficacy, and Safety

TL;DR: This chapter will review the mechanisms of action of heparin and LMWHs, their pharmacokinetics, anticoagulant effects, side effects, and laboratory monitoring, and the results of clinical trials will be discussed.
Journal ArticleDOI

Heparin and Low-Molecular-Weight Heparin: The Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy

Jack Hirsh, +1 more
- 01 Sep 2004 - 
TL;DR: It has been determined that UFH infusion is preferable to LMWH injection in patients with creatinine clearance of < 25 mL/min, until further data on therapeutic dosing of LMWHs in renal failure have been published.
References
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Journal ArticleDOI

A modified uronic acid carbazole reaction

TL;DR: It has been found possible to distinguish betweenHeparin, heparin derivatives, and other polyuronides of connective tissue by comparing the effect of chlorides on the color yield in both procedures by modifying Dische's carbazole reaction for uronic acid in the presence of borate.
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The Purification and Mechanism of Action of Human Antithrombin-Heparin Cofactor

TL;DR: It is suggested that heparin binds to the inhibitor and causes a conformational change which results in a more favorable exposure of the arginine reactive site, allowing a rapid interaction with thrombin.
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Mechanism of the anticoagulant action of heparin

TL;DR: The bulk of the evidence available indicates that binding of heparin to the protease alone cannot be responsible for the accelerating effect of the polysaccharide on the antithrombin-protease reaction, and thus the anticoagulant activity.
Journal ArticleDOI

Further characterization of the antithrombin-binding sequence in heparin.

TL;DR: It is concluded that the antithrombin binding site in heparin is represented by the pentasaccharide sequence extending from unit 2 to unit 6 of the octasacCharide studied, and the results suggest that the 6-sulfate group in unit 2 may be involved in antithrubin binding.
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The structure of heparin oligosaccharide fragments with high anti-(factor Xa) activity containing the minimal antithrombin III-binding sequence. Chemical and 13C nuclear-magnetic-resonance studies.

TL;DR: The chemical composition and the 13C n.r.p.m. spectra of heparin oligosaccharides, having high affinity for antithrombin III and high anti-(Factor Xa) activity, prepared by three independent approaches, have been studied and compared with those of the corresponding inactive species.
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