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  • Title: Efficient targeted anticoagulant with active RGD motif.
    Author: Bi Q, Zhou X, Cen X, Qu H, Luo J, Huang Y, Zhu S.
    Journal: Thromb Res; 2007; 120(4):541-7. PubMed ID: 17222892.
    Abstract:
    Three anticoagulants combining large peptide recombinant hirudin variants (rHV2-K47) and Arg-Gly-Asp (RGD) motif related to platelet aggregation were generated, i.e. sequences CRFPRGDADPYCE and CNPRGDFRCI were added to the C-terminus of hirudin to obtain RGD-hirudin 1 and 2, respectively, and the sequence RGDSE was inserted between residues 53-54 of hirudin to obtain RGD-hirudin 3. All products exhibited antithrombin and antiplatelet activities, especially IC50 of RGD-hirudin 1 and 2 were much lower with respect to previously reported similar peptides. Our data suggested that RGD-hirudin 1 and 2 would be promising anticoagulants in clinic. Moreover, the triangular structure of active RGD was shown by computer simulation, which might contribute to our understanding on integrin-related peptides and proteins.
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