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Synthesis of a Pentasaccharide–Oligonucleotide Conjugate: A Novel Antithrombotic Agent

✍ Scribed by Rogier C. Buijsman; Dr. Ir. Will H. A. Kuijpers; Jan E. M. Basten; Dr. Esther Kuyl-Yeheskiely; Dr. Gijsbert A. van der Marel; Prof. Dr. Constant A. A. van Boeckel; Prof. Dr. Jacques H. van Boom

Publisher
John Wiley and Sons
Year
1996
Tongue
English
Weight
673 KB
Volume
2
Category
Article
ISSN
0947-6539

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✦ Synopsis

Derivatization of the octadecathymidylate derivative 18 (T18 ODN) containing a free amine function with sulfo-SIAB@ gave the corresponding iodoacetyl ODN 21. Conjugation of the latter with the thiol-containing pentasaccharide 17c gave pentasaccharide-ODN conjugate 111, which exhibited anti-Xa and antithrombin activities of 173 Umg-' and 5 Umg-I, respectively.

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