| abstract |
The isolated and purified PAI from several 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 formulaR12 N(CH 2)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: 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 O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa. |