Synthesis of a pentasaccharide-oligonucleotide conjugate: A novel antithrombotic agent

Derivatization of the octadecathymidylate derivative 18 (T-18 ODN) containing a free amine function with sulfo-SIAB(R) gave the corresponding iodoacetyl ODN 21. Conjugation of the latter with the thiol-containing pentasaccharide 17c gave pentasaccharide-ODN conjugate III, which exhibited anti-Xa and...

Full description

Saved in:
Bibliographic Details
Published inChemistry : a European journal Vol. 2; no. 12; pp. 1572 - 1577
Main Authors Buijsman, RC, Kuijpers, WHA, Basten, JEM, KuylYeheskiely, E, vanderMarel, GA, vanBoeckel, CAA, vanBoom, JH
Format Journal Article
LanguageEnglish
Published WEINHEIM Wiley 01.12.1996
Subjects
Chemistry
Chemistry, Multidisciplinary
Physical Sciences
Science & Technology
ACCELERATION
protecting groups
ASSAY
THROMBIN
ANALOGS
oligosaccharides
oligonucleotides
enzyme inhibitors
HEPARIN
FACTOR-XA
antithrombotics
Online AccessGet more information

Cover

More Information
Summary:Derivatization of the octadecathymidylate derivative 18 (T-18 ODN) containing a free amine function with sulfo-SIAB(R) gave the corresponding iodoacetyl ODN 21. Conjugation of the latter with the thiol-containing pentasaccharide 17c gave pentasaccharide-ODN conjugate III, which exhibited anti-Xa and antithrombin activities of 173 U mg(-1) and 5 U mg(-1), respectively.
ISSN:0947-6539
DOI:10.1002/chem.19960021216