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Synthesis of oligomeric assemblies of a platelet-binding key disaccharide in heparin and their biological activities

✍ Scribed by Shuhei Koshida; Yasuo Suda; Michael Sobel; Shoichi Kusumoto


Book ID
104211371
Publisher
Elsevier Science
Year
2001
Tongue
French
Weight
92 KB
Volume
42
Category
Article
ISSN
0040-4039

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✦ Synopsis


Heparin, highly sulfated glycosaminoglycan, binds to platelets. A key disaccharide unit in heparin was previously found to be responsible for the binding, and the frequency of the disaccharide unit was important for the binding potency. A newly developed method based on the reductive amination was effectively applied to prepare structurally defined oligomeric assemblies possessing multiple units of the key disaccharide. From their platelet-binding activities measured by the competitive binding assay, the enhancement of the activity was clearly observed with increasing number of the key disaccharide.


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A key disaccharide unit in heparin, O-(2-deoxy-2-sulfamido-6-O-sulfo-a-D-glucopyranosyl)-(1---.4)-2-O-sulfo-Ot-L-idopyranosyluronic acid, was previously found to be responsible for the binding interaction of heparin to platelets. A clustering effect to enhance the binding was found to be dependent o