Method of inhibiting and inducing human platelet aggregation

Details Method of inhibiting and inducing human platelet aggregation Method of inhibiting and inducing human platelet aggregation

1984-04-10

1987-04-28

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 16, 530326, C07K 708, A61K 3702

Patent

active

046614710

ABSTRACT:
A method of inhibiting thrombin or ADP-induced human platelet aggregation by fibrinogen 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 fibrinogen, a plasma protein necessary for platelet aggregation. The method of the invention is useful for inhibiting of the formation of hemostatic platelet plugs and of 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 formation of thrombin or ADP-modified platelet aggregates by administration of a synthetic aggregating molecule which represents a functional substitute for fibrinogen.

REFERENCES:
patent: 4303592 (1981-12-01), Laura et al.
patent: 4351337 (1982-09-01), Sidman
patent: 4455290 (1984-06-01), Olepa et al.
patent: 4476116 (1984-10-01), Anik
"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).
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.

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