| 摘要 |
The invention provides heparin preparations of desired balance in anticoagulant activity and ability to inhibit vWF-mediated platelet adhesion/aggregation, and peptides useful in obtaining and identifying them. The invention thus provides a peptide of the formula: B1X2B3B4B5X6X7X8X9B10B11X12, wherein each B is independently a basic amino acid and each X is independently a nonbasic amino acid, wherein any of said peptides is optionally extended at the N- or C-terminus by moieties which do not interfere with the affinity of the peptide for heparin; and wherein one or more of the peptide linkages may optionally be replaced by an isosteric linkage, which peptide specifically binds a fraction of heparin preparations. The peptide is useful as a pharmaceutical composition to interfere with heparin inhibition of platelet aggregation or adhesion as well as to obtain fractions of heparin or derivatives thereof which are enhanced or depleted in ability to inhibit platelet aggregation and adhesion, dependent on von Willebrand Factor. The resulting heparin subfractions are useful pharmaceutically to regulate blood clotting that is dependent on platelet aggregation/adhesion. |
