Method of inhibiting binding of von Willebrand factor to human p

Details Method of inhibiting binding of von Willebrand factor to human p Method of inhibiting binding of von Willebrand factor to human p

1984-04-10

1987-05-19

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 17, A61K 3743

Patent

active

046668845

ABSTRACT:
A method of inhibiting von Willebrand factor binding to human platelets induced with thrombin, ADP, or other stimuli has been developed. The administration of the small molecular weight peptide or the synthetic inhibitory molecule of the invention significantly inhibits thrombin or ADP-modified human platelets binding of von Willebrand factor, a plasma protein necessary for platelet interaction with blood vessels. The method of the invention is useful for inhibiting the formation of hemostatic platelet plugs and the initiation of thrombotic lesions. The blockage caused by hemostatic platelet plugs and the damage caused by thrombotic lesions are major factors in heart disease and stroke. The invention also includes a method of inducing the interaction of platelets with blood vessels by administration of a synthetic platelet reactive molecule.

REFERENCES:
patent: 4303592 (1981-12-01), Laura et al.
patent: 4351337 (1982-09-01), Sidman
patent: 4455290 (1984-06-01), Olexa et al.
patent: 4476116 (1984-10-01), Anik
Biochemistry, 1982, vol. 21, No. 6, pp. 1414-1420--Isolation, Characterization and Synthesis of Peptides from Human Fibrinogen that Block the Staphylococcal Clumping Reaction and Construction of a Synthetic Particle.
Biochemical and Biophysical Research Communications, vol. 107, No. 1, Jul. 16, 1982, pp. 181-187--Localization of a Site Interacting with Human Platelet Receptor on Carboxy-Terminal Segment of Human Fibrinogen Chain.
Thrombosis Research 29; 249-255, 1983--Fibrinogen Site for Platelets.
"Localization of a Fibrin .alpha.-Chain Polymerization Site Within Segment Thr-374 to Glu-396 of Human Fibrinogen", Proc. Natl. Ac. Sci. (USA) 81, pp. 5980-5984 (1984).

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