Platelet aggregation inhibitors

Details Platelet aggregation inhibitors Platelet aggregation inhibitors

C - Chemistry, Metallurgy

12

N

C12N 15/12 (2006.01) A61K 38/12 (2006.01) A61K 38/17 (2006.01) A61K 38/36 (2006.01) A61K 38/57 (2006.01) C07K 14/435 (2006.01) C07K 14/46 (2006.01) C07K 14/75 (2006.01) C07K 14/755 (2006.01) C07K 14/78 (2006.01) G01N 33/566 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2059124

An assay for screening snake venom for the pres- ence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accom- plished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formula R1 2 N(CH2)4CHNHCO- wherein each R1 is independently H, alkyl(1-6C) or at most one R1 is R2-C=NR3 wherein R2 is H, alkyl(1-6C), phenyl or benzyl, or is NR4 2 in which each R4 is independently H or alkyl(1-6C) and R3 is H, alkyl(1-6C), phenyl or benzyl, or R2-C=NR3 is a radical selected from the group consisting of: Image where m is an integer of 2-3, and each R5 is independently H or alkyl(1-6C); and wherein one or two (CH2) may be replaced by 0 or S provided said O or S is not adjacent to another heteroatom -101- are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

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