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aIIbb3 and Its Antagonism at the New Millennium

Journal: Thrombosis and Haemostasis
ISSN: 0340-6245
Issue: 2001: 86/1 (July, State of the Art) pp.1-508
Pages: 34-40

aIIbb3 and Its Antagonism at the New Millennium

Edward F. Plow (1) , Czeslaw S. Cierniewski (2) , Zihui Xiao (1) , Thomas A. Haas (1) , Tatiana V. Byzova (1)
(1) Joseph J. Jacobs Center for Thrombosis and Vascular Biology, Department of Molecular Cardiology, Cleveland Clinic Foundation, Cleveland, OH, USA, (2) Department of Biophysics, Medical University in Lodz, Lodz, Poland


Because of its major role in regulating platelet functions and its prominence on the cell surface, integrin aIIbb3 has been the subject of intensive investigations. Such studies have provided substantial insights into its structure-function relationships and have led to the development of anti-thrombotic drugs that target the receptor. Nevertheless, recent findings have indicated that our understanding of the structure and function of aIIbb3 remains inadequate. This article addresses two aspects of still evolving aIIbb3 function: 1) the interface between aIIbb3 and the blood coagulation system, resulting from interaction of prothrombin with the receptor; and 2) the molecular basis for recognition of the RGD and the fibrinogen g-chain peptide ligands by aIIbb3. As illustrated by these two examples, there is still much to be learned about aIIbb3 if we are to fully appreciate its functions and its potential as a therapeutic target.