Synthesis of Tailor‐Made Glycoconjugates Showing AT III‐Mediated Inhibition of Blood Coagulation Factors Xa and Thrombin | Zendy

Westerduin Pieter | Zendy; Basten Jan E. M. | Zendy; Broekhoven Marc A. | Zendy; de Kimpe Vera | Zendy; Kuijpers Will H. A. | Zendy; van Boeckel Constant A. A. | Zendy

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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.

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