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Synthesis of Tailor‐Made Glycoconjugates Showing AT III‐Mediated Inhibition of Blood Coagulation Factors Xa and Thrombin
Author(s) -
Westerduin Pieter,
Basten Jan E. M.,
Broekhoven Marc A.,
de Kimpe Vera,
Kuijpers Will H. A.,
van Boeckel Constant A. A.
Publication year - 1996
Publication title -
angewandte chemie international edition in english
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 0570-0833
DOI - 10.1002/anie.199603311
Subject(s) - glycoconjugate , antithrombin , thrombin , coagulation , chemistry , heparin , thrombin generation , biochemistry , platelet , biology , immunology , medicine
A sufficiently long spacer between the antithrombin‐ and thrombin‐binding domains (ABD and TBD, respectively) is necessary to impart antithrombin activity to a synthetic glycoconjugate (shown schematically below). The spacer need not consist of multiple sugar units as in heparin; a simple chain about 50 atoms in length suffices. In addition, varying the charge density of the TBD affects the inhibitor activity, and symmetric glycoconjugates (TBD = ABD) also display high antithrombin activities.