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Identification of a hexasaccharide sequence able to inhibit thrombin and suitable for 'polymerisation'
P Duchaussoy1, G Jaurand, P A Driguez
1Sanofi Recherche, Haemobiology Research Department, Toulouse, France.
Carbohydrate Research
|August 31, 1999
Summary
Researchers synthesized three hexasaccharides with varying antithrombin affinities. One specific compound, derived from a single precursor, shows promise as a heparin mimetic for inhibiting thrombin and Factor Xa.
Area of Science:
- Carbohydrate Chemistry
- Biochemistry
- Medicinal Chemistry
Background:
- Heparin and its derivatives are crucial anticoagulants.
- Developing synthetic heparin mimetics is essential for therapeutic applications.
- Understanding structure-activity relationships is key for designing effective inhibitors.
Purpose of the Study:
- To synthesize novel hexasaccharides with potential antithrombin activity.
- To evaluate the affinity of synthesized compounds for antithrombin.
- To identify simple oligosaccharidic heparin mimetics for inhibiting coagulation factors.
Main Methods:
- Synthesis of hexasaccharides using disaccharide building block precursors.
- Purification and characterization of the synthesized compounds.
- Affinity assessment for antithrombin.
Main Results:
- Three hexasaccharides with low to very high affinity for antithrombin were successfully synthesized.
- One hexasaccharide, derived from a single disaccharide precursor, demonstrated significant potential.
- This compound serves as a starting point for developing heparin mimetics.
Conclusions:
- Synthetic hexasaccharides can effectively mimic heparin's anticoagulant properties.
- A specific hexasaccharide shows promise for inhibiting thrombin and Factor Xa.
- This research paves the way for simplified heparin mimetic drug development.