Related Experiment Video
Updated: Jul 6, 2026

Ferric Chloride-induced Murine Thrombosis Models
Published on: September 5, 2016
"Mirror image" antagonists of thrombin-induced platelet activation based on thrombin receptor structure
D T Hung1, T K Vu, V I Wheaton
1Department of Medicine, University of California, San Francisco 94143.
Abstract:
Platelet activation by thrombin plays a critical role in hemostasis and thrombosis. Based on structure-activity studies of a cloned platelet thrombin receptor, we designed two "mirror image" antagonists of thrombin and thrombin receptor function. First, "uncleavable" peptides mimicking the receptor domain postulated to interact with thrombin were found to be potent thrombin inhibitors. Second, proteolytically inactive mutant thrombins designed to bind but not cleave the thrombin receptor were found to be specific antagonists of receptor activation by thrombin. The effectiveness of these designed antagonists in blocking thrombin-induced platelet activation suggests a model for thrombin-receptor interaction and possible strategies for the development of novel antithrombotic agents.
Related Concept Videos
Receptor Tyrosine Kinases
Intracellular Signaling Affects Focal Adhesions
Some...
Anticoagulant Drugs: Low-Molecular-Weight Heparins
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Clot Retraction and Fibrinolysis

